scholarly journals Synthesis and Anticancer Activity of Novel Amide Tagged Trifluoromethyl Indole and Pyrimido Indole Derivatives

2021 ◽  
Vol 33 (10) ◽  
pp. 2327-2332
Author(s):  
Manoj Kumar Mandadi ◽  
Ramana Reddy Bobbala ◽  
Balakrishna Kolli ◽  
Rambabu Gundla
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Anticancer Activity ◽  
Human Cancer ◽  
Indole Derivatives ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Micromolar Concentration ◽  
A549 Lung

A series of novel amide tagged trifluoromethyl indole and pyrimido indole derivatives 4a-e & 5a-e and 6a-d & 7a-d were synthesized from 4-methyl-2-(methylamino)-6-(trifluoromethyl)isophthalonitrile (1) on reaction with bromoethyl acetate to obtain 2a and 2b isomers. Compound 2a treated with hydrazine hydrate followed by Schiff base reaction to get compounds 4a-e. In another way, compound 2a on reaction with aliphatic primary amine to get compounds 6a-d. For cyclization, compounds 4a-e & 6a-d treated with trifluoroacetic acid to obtain compounds 5a-e and 7a-d, respectively. All the synthesized compounds 4a-e & 5a-e and 6a-d & 7a-d were tested for anticancer activity against four human cancer cell lines such as A549-lung cancer (CCL-185), MCF7-breast cancer (HTB-22), DU145-prostate cancer (HTB-81) and HeLa-cervical cancer (CCL-2). Compounds 9e and 9f were found to have promising anticancer activity at micromolar concentration.

Design, Synthesis and Biological Evaluation of 3-(3,4,5-Trimethoxyphenyl)- 5-(2-(5-arylbenzo[b]thiophen-3-yl)oxazol-5-yl)isoxazole Derivatives as Anticancer Agents

2020 ◽  
Vol 17 (5) ◽  
pp. 345-351
Author(s):  
Syndla Premalatha ◽  
G. Rambabu ◽  
Islavathu Hatti ◽  
Dittakavi Ramachandran
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Isoxazole Derivatives

A new series of 3-(3,4,5-trimethoxyphenyl)-5-(2-(5-arylbenzo[b]thiophen-3-yl)oxa zol-5- yl)isoxazole derivatives were designed and synthesized. All these derivatives were evaluated for their anticancer activity against various human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer)-four human cancer cell lines by using MTT assay. Here, etoposide was used as a standard reference drug and most of the compounds were exhibited good anticancer activity with respect to cell lines. Among all compounds, five compounds 11b, 11c, 11f, 11i and 11j showed more potent activity than standard drug, in which, compound 11f was the most promising compound.

Design, Synthesis and Anticancer Evaluation of 1,2,4-Oxadiazole Bearing Isoxazole-Pyrazole Derivatives

2020 ◽  
Vol 17 (5) ◽  
pp. 352-359 ◽  
Author(s):  
Bhukya Ravinaik ◽  
Dittakavi Ramachandran ◽  
Mandava Venkata Basaveswara Rao
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Human Cancer ◽  
Pyrazole Derivatives ◽  
Human Cancer Cell ◽  
Design Synthesis ◽  
Standard Drug ◽  
Human Cancer Cell Lines ◽  
A549 Lung ◽  
Mcf 7

A novel library of 1,2,4-oxadiazole bearing isoxazole-pyrazole derivatives (13a-j) were designed, synthesized and evaluated for their anticancer activity towards MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer) human cancer cell lines by MTT assay. Here etoposide used as standard drug. Among them, five compounds (13b, 13c, 13d, 13h and 13i) were exhibited more potent activity. In which compound 13h was the most promising compound against all cell lines MCF-7, A549, DU-145 and MDA MB-231.

Synthesis and Cytotoxicity Evaluation of Some Novel 1-(3-Chlorophenyl)piperazin-2-one Derivatives Bearing Imidazole Bioisosteres

2013 ◽  
Vol 66 (6) ◽  
pp. 655 ◽  
Author(s):  
Saeed Ghasemi ◽  
Simin Sharifi ◽  
Soodabeh Davaran ◽  
Hosein Danafar ◽  
Davoud Asgari ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Lines ◽  
Human Cancer ◽  
Imidazole Ring ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines ◽  
Bioisosteric Replacement ◽  
Ht 29 ◽  
Ftase Inhibitor ◽  
A549 Lung

A series of substituted 3-chlorophenylpiperazinone derivatives were synthesised using L-778123 (an imidazole-containing FTase inhibitor) as a model by bioisosteric replacement of the imidazole ring. The final compounds were evaluated against two human cancer cell lines including A549 (lung cancer) and HT-29 (colon cancer) by MTT assay. The results showed that substitution of imidazole ring with 1-amidinourea, semicarbazide, and thiobiuret led to improvement of cytotoxic activity against both cell lines.

Synthesis of novel N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives as inducers of apoptosis in MCF-7 breast cancer cells

RSC Advances ◽  
2016 ◽  
Vol 6 (19) ◽  
pp. 15286-15297 ◽  
Author(s):  
Manjunath G. Sunagar ◽  
Supreet Gaonkar ◽  
Santosh G. Sunagar ◽  
Narahari Deshapande ◽  
Ningaraddi S. Belavagi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Breast Cancer Cells ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Purine Derivatives ◽  
Human Cancer Cell Lines ◽  
Mcf 7

A series of N-9 substituted 6-(4-(4-propoxyphenyl)piperazin-1-yl)-9H-purine derivatives (PP05–PP21) were prepared and evaluated for their anticancer activity against a panel of human cancer cell lines.

scholarly journals Synthesis and Cytotoxic Activity Study of Novel 2-(Aryldiazenyl)-3-methyl-1H-benzo[g]indole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4240
Author(s):  
Manar M. Arafeh ◽  
Ebrahim Saeedian Moghadam ◽  
Sirin A. I. Adham ◽  
Raphael Stoll ◽  
Raid J. Abdel-Jalil
Keyword(s):  
Melting Point ◽  
Cytotoxic Activity ◽  
Elemental Analysis ◽  
13C Nmr ◽  
National Cancer Institute ◽  
Polyphosphoric Acid ◽  
Human Cancer ◽  
Indole Derivatives ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a–f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a–f) were characterized using 1H NMR, 13C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.

scholarly journals Pheophorbide a: State of the Art

Marine Drugs ◽  
2020 ◽  
Vol 18 (5) ◽  
pp. 257 ◽  
Author(s):  
Assunta Saide ◽  
Chiara Lauritano ◽  
Adrianna Ianora
Keyword(s):  
Clinical Trials ◽  
Photodynamic Therapy ◽  
Anticancer Activity ◽  
State Of The Art ◽  
Human Cancer ◽  
Human Cancer Cell ◽  
Pheophorbide A ◽  
Human Cancer Cell Lines ◽  
Chlorophyll Breakdown ◽  
Chlorophyll Derivative

Chlorophyll breakdown products are usually studied for their antioxidant and anti-inflammatory activities. The chlorophyll derivative Pheophorbide a (PPBa) is a photosensitizer that can induce significant anti-proliferative effects in several human cancer cell lines. Cancer is a leading cause of death worldwide, accounting for about 9.6 million deaths, in 2018 alone. Hence, it is crucial to monitor emergent compounds that show significant anticancer activity and advance them into clinical trials. In this review, we analyze the anticancer activity of PPBa with or without photodynamic therapy and also conjugated with or without other chemotherapic drugs, highlighting the capacity of PPBa to overcome multidrug resistance. We also report other activities of PPBa and different pathways that it can activate, showing its possible applications for the treatment of human pathologies.

Synthesis of novel amide and Schiff’s base functionalized novel pyrido[1,2-a] pyrimidin-4-one derivatives and their anticancer activity studies.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sailu Betala ◽  
Chiranjeevi Abba ◽  
Hanumandlu Racha
Keyword(s):  
Anticancer Activity ◽  
Hydrazine Hydrate ◽  
Human Cancer ◽  
Aromatic Aldehydes ◽  
Human Cancer Cell ◽  
Hep G2 ◽  
Schiff’S Base ◽  
Human Cancer Cell Lines ◽  
Amide Derivatives ◽  
Mcf 7

Abstract: A series of novel amide and Schiffs base functionalized novel pyrido[1,2-a]pyrimidin-4-one derivatives were prepared starting from 6-(thiophene-2-yl)/phenyl-4-(trifluoromethyl) pyridin-2-amine 1a and 1b. These compounds on reaction with EMME, to afford compounds 2a and 2b, followed by cyclization to afford compounds 3a and 3b. Treatment of compound 3a and 3b with hydrazine hydrate to get compounds 4a and 4b, compounds 4a and 4b on reaction with different substituted aromatic aldehydes to get Schiff’s base derivatives 5a-j, in another way compounds 3a, 3b on reaction with aliphatic amines to get amide derivatives 6a-f. All the compounds 5a-j and 6a-f were screened against four human cancer cell lines (HeLa, COLO205, Hep G2, and MCF 7), among all the derivatives, compounds 5c, 5e, 6a, and 6b showed promising anticancer activity.

Indole based prostate cancer agents

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Sunil Kumar ◽  
Madhuri T. Patil ◽  
Deepak B. Salunke
Keyword(s):  
Breast Cancer ◽  
Prostate Cancer ◽  
Lung Cancer ◽  
Immune System ◽  
Anticancer Agents ◽  
Crucial Role ◽  
Heterocyclic Compounds ◽  
Indole Derivatives ◽  
Cancer Chemotherapeutics ◽  
Privileged Structure

Abstract Cancer weakens the immune system which fails to fight against the rapidly growing cells. Among the various types of cancers, prostate cancer (PCa) is causing greater number of deaths in men after lung cancer, demanding advancement to prevent, detect and treat PCa. Several small molecule heterocycles and few peptides are being used as oncological drugs targeting PCa. Heterocycles are playing crucial role in the development of novel cancer chemotherapeutics as well as immunotherapeutics. Indole skeleton, being a privileged structure has been extensively used for the discovery of novel anticancer agents and the application of indole derivatives against breast cancer is well documented. The present article highlights the usefulness of indole linked heterocyclic compounds as well as the fused indole derivatives against prostate cancer.

scholarly journals Colchicine: Isolation, LC–MS QTof Screening, and Anticancer Activity Study of Gloriosa superba Seeds

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2772 ◽  
Author(s):  
Balkrishna ◽  
Das ◽  
Pokhrel ◽  
Joshi ◽  
Laxmi ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Human Cancer ◽  
Cell Cytotoxicity ◽  
Human Cancer Cell ◽  
Gloriosa Superba ◽  
Human Cancer Cell Lines ◽  
Insight Into ◽  
Mb231 Cell ◽  
Mcf 7

Colchicine was extracted from Gloriosa superba seeds using the Super Critical Fluid (CO2) Extraction (SCFE) technology. The seeds were purified upto 99.82% using column chromatography. Colchicine affinity was further investigated for anticancer activity in six human cancer cell lines, i.e., A549, MCF-7, MDA-MB231, PANC-1, HCT116, and SiHa. Purified colchicine showed the least cell cytotoxicity and antiproliferation and caused no G2/M arrest at clinically acceptable concentrations. Mitotic arrest was observed in only A549 and MDA-MB231 cell lines at 60nM concentration. Our finding indicated the possible use of colchicine at a clinically acceptable dose and provided insight into the science behind microtubule destabilization. However, more studies need to be conducted beforethese findings could be established.

Effect of the Method of Preparation on the Composition and Cytotoxic Activity of the Essential Oil of Pituranthos tortuosus

2011 ◽  
Vol 66 (3-4) ◽  
pp. 143-148 ◽  
Author(s):  
Hossam M. Abdallah ◽  
Shahira M. Ezzat
Keyword(s):  
Breast Cancer ◽  
Essential Oil ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Line ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Human Cancer Cell Lines

The aerial parts of Pituranthos tortuosus (Desf.) Benth and Hook (Apiaceae), growing wild in Egypt, yielded 0.8%, 0.6%, and 1.5% (v/w) of essential oil when prepared by hydrodistillation (HD), simultaneous hydrodistillation-solvent (n-pentane) extraction (Lickens- Nickerson, DE), and conventional volatile solvent extraction (preparation of the “absolute”, SE), respectively. GC-MS analysis showed that the major components in the HD sample were β-myrcene (18.81%), sabinene (18.49%), trans-iso-elemicin (12.90%), and terpinen- 4-ol (8.09%); those predominent in the DE sample were terpinen-4-ol (29.65%), sabinene (7.38%), γ-terpinene (7.27%), and β-myrcene (5.53%); while the prominent ones in the SE sample were terpinen-4-ol (15.40%), dill apiol (7.90%), and allo-ocimene (4E,6Z) (6.00%). The oil prepared in each case was tested for its cytotoxic activity on three human cancer cell lines, i.e. liver cancer cell line (HEPG2), colon cancer cell line (HCT116), and breast cancer cell line (MCF7). The DE sample showed the most potent activity against the three human cancer cell lines (with IC50 values of 1.67, 1.34, and 3.38 μg/ml against the liver, colon, and breast cancer cell lines, respectively). Terpinen-4-ol, sabinene, γ-terpinene, and β-myrcene were isolated from the DE sample and subjected to a similar evaluation of cytotoxic potency; signifi cant activity was observed

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