scholarly journals DESIGN, SYNTHESIS AND ANTICANCER ACTIVITY OF STRUCTURALLY MODIFIED 1, 3, 4-OXADIAZOLE INCORPORATED 2H-CHROMENE DERIVATIVES AS ANTICANCER AGENTS

2019 ◽  
Vol 10 (10) ◽  
pp. 87-92
Author(s):  
Radha Krishna Muniganti ◽  
H V Jayaprakash
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Design Synthesis

Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Sar Study

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents

2021 ◽  
Author(s):  
Guddeti Dileep Kumar ◽  
Bandi Siva ◽  
Sravanthi Vadlamudi ◽  
Surendar Reddy Bathula ◽  
Hashnu Dutta ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Traditional Medicinal Plants ◽  
Aloe Emodin ◽  
Synthesis And Biological Evaluation

In connection with our continuous efforts to generate new derivatives from lead compounds isolated from traditional medicinal plants, a series of aloe-emodin derivatives were synthesized and assessed for potential anticancer activity against a panel of cancer cell lines.

Design, Synthesis and Evaluation of Hybrid 2-Heteroaryl BenzimidazoleChalcone Derivatives as Anticancer Agents

2020 ◽  
Vol 17 ◽  
Author(s):  
Gajula Shyam Kumar ◽  
Bethi Rathnakar ◽  
Sridhar Gattu ◽  
Surender Singh Jadav ◽  
Nimma Rameshwar ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Phenyl Ring ◽  
Human Breast ◽  
Design Synthesis ◽  
Abl Tyrosine Kinase ◽  
Ovarian Cancer Cell Lines ◽  
Methoxy Groups ◽  
Ic50 Values ◽  
Human Breast Carcinoma Cells

: A series of 2-heteroaryl benzimidazole-chalcone hybrids were synthesized and the anticancer activity was estimated by MTT assay in human breast, lung, colon, and ovarian cancer cell lines. The biological results indicate that the compounds showed good anticancer activity with a range of IC50 values 0.056-19.5 µM. Compound 11b with hexa methoxy groups, bearing three methoxy groups on each terminal aryl ring exhibited a significant IC50 value (56 nM) against human breast carcinoma cells, which is 37 times higher potency in comparison with the reference Etoposide. Further compounds substituted variably with methoxy and nitro groups on the phenyl ring of chalcone showed more promising anticancer activity than the compounds with unsubstituted phenyl ring or variably alkyl-substituted phenyl ring of chalcone. The molecular docking results indicate that the synthesized compounds bind in the active site of Abl tyrosine kinase, the target of anticancer drug Imatinib. The present study provides the synergistic effect of hybrids, benzimidazole-chalcones as potential anticancer agents and will aid in the discovery of new anticancer agents.

2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line

2019 ◽  
Vol 19 (13) ◽  
pp. 1080-1092 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Antimicrobial Studies ◽  
Development Of Resistance ◽  
Microbial Infections ◽  
New Chemical Entities

Background: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer. Objective: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole. Methods: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and Sulforhodamine-B (SRB) assay, respectively. Results: Compounds 8 (MICpa, an = 2.41, 1.20 µM/ml), 10 (MICse, sa = 2.50 µM/ml), 20 (MICec = 2.34 µM/ml) and 25 (MICca = 1.46 µM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 µg/ml) and 23 (IC50 = 7 µg/ml) exhibited significant anticancer activity. Conclusion: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead molecules for the development of novel antifungal agents.

scholarly journals Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives

MedChemComm ◽  
2017 ◽  
Vol 8 (1) ◽  
pp. 176-183 ◽  
Author(s):  
Radhakrishnam Raju Ruddarraju ◽  
Adharvana Chari Murugulla ◽  
Ravindar Kotla ◽  
Muni Chandra Babu Tirumalasetty ◽  
Rajendra Wudayagiri ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Docking Studies ◽  
Design Synthesis ◽  
Amide Derivatives

A new series of theophylline analogues containing 1,2,3-triazoles with different amide groups (22–41) has been designed and synthesized, and their biological activities have been evaluated as potential anticancer agents.

Design, synthesis and mechanism of novel shikonin derivatives as potent anticancer agents

RSC Advances ◽  
2015 ◽  
Vol 5 (40) ◽  
pp. 31759-31767 ◽  
Author(s):  
Shahla Karim Baloch ◽  
Lin Ma ◽  
Xue-Liang Wang ◽  
Jing Shi ◽  
Yu Zhu ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Activity ◽  
Cell Cycle Arrest ◽  
Anticancer Agents ◽  
Design Synthesis ◽  
Cycle Arrest ◽  
Shikonin Derivatives ◽  
M Phase

Novel shikonin derivatives were synthesised and probed as anticancer agents. Compound 40 showed the best anticancer activity with an IC50 of 1.26 μM, could induce apoptosis and cause cell cycle arrest at the G2/M phase via the P21 p-CDC2 (Tyr15) pathway independent of P53.

Design, synthesis and structure-activity relationship studies of novel spirochromanone hydrochloride analogs as anticancer agents

2022 ◽  
Author(s):  
Surendar Chitti ◽  
Sravani Pulya ◽  
Adinarayana Nandikolla ◽  
Tarun Kumar Patel ◽  
Karan Kumar Banoth ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Growth Factor Receptor ◽  
Docking Study ◽  
Kinase Domain ◽  
Molecular Docking Study ◽  
Design Synthesis ◽  
Hek 293 ◽  
B16f10 Cells ◽  
Mcf 7

Aim: Literature reports suggest spirochromanone derivatives exhibit anticancer activity. Methodology: The authors designed and synthesized 18 spirochromanone derivatives (Csp 1–18). The compounds were characterized and evaluated for anticancer activity against human breast cancer (MCF-7) and murine melanoma (B16F10) cell lines. Results: The anticancer activity ranged from 4.34 to 29.31 μm. The most potent compounds, Csp 12 and Csp 18, were less toxic against the human embryonic kidney (HEK-293) cell line and ∼ two/∼four fold selective toward MCF-7 than B16F10 in comparison to the reference, BG-45. Csp 12 caused 28.6% total apoptosis, leading to significant cytotoxicity, and arrested the G2 phase of the cell cycle in B16F10 cells. A molecular docking study of Csp 12 exhibited effective binding at the active site of the epidermal growth factor receptor kinase domain. Conclusion: This study highlights the importance of spirochromanones as anticancer agents.

scholarly journals Design, Synthesis, and Anticancer Activity Studies of Novel Quinoline-Chalcone Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4899
Author(s):  
Yong-Feng Guan ◽  
Xiu-Juan Liu ◽  
Xin-Ying Yuan ◽  
Wen-Bo Liu ◽  
Yin-Ru Li ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Ros Generation ◽  
Dependent Manner ◽  
Gastric Cancer Cells ◽  
Design Synthesis ◽  
Chalcone Derivatives ◽  
Ic50 Values ◽  
Hct 116 ◽  
Mcf 7

The chalcone and quinoline scaffolds are frequently utilized to design novel anticancer agents. As the continuation of our work on effective anticancer agents, we assumed that linking chalcone fragment to the quinoline scaffold through the principle of molecular hybridization strategy could produce novel compounds with potential anticancer activity. Therefore, quinoline-chalcone derivatives were designed and synthesized, and we explored their antiproliferative activity against MGC-803, HCT-116, and MCF-7 cells. Among these compounds, compound 12e exhibited a most excellent inhibitory potency against MGC-803, HCT-116, and MCF-7 cells with IC50 values of 1.38, 5.34, and 5.21 µM, respectively. The structure–activity relationship of quinoline-chalcone derivatives was preliminarily explored in this report. Further mechanism studies suggested that compound 12e inhibited MGC-803 cells in a dose-dependent manner and the cell colony formation activity of MGC-803 cells, arrested MGC-803 cells at the G2/M phase and significantly upregulated the levels of apoptosis-related proteins (Caspase3/9 and cleaved-PARP) in MGC-803 cells. In addition, compound 12e could significantly induce ROS generation, and was dependent on ROS production to exert inhibitory effects on gastric cancer cells. Taken together, all the results suggested that directly linking chalcone fragment to the quinoline scaffold could produce novel anticancer molecules, and compound 12e might be a valuable lead compound for the development of anticancer agents.

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