scholarly journals Synthesis and Cytotoxic Studies of Pyrrolopyrimidine Derivatives

2021 ◽  
Vol 33 (8) ◽  
pp. 1855-1860
Author(s):  
Rangaswamy Roopashree ◽  
Toreshettahally R. Swaroop ◽  
Chalya M. Shivaprasad ◽  
Swamy Jagadish ◽  
Kanchugarakoppal S. Rangappa
Keyword(s):  
Cytotoxic Activity ◽  
In Vitro Cytotoxicity ◽  
Benzyl Amine ◽  
Cytotoxic Studies ◽  
Derivatives Of

The synthesis and in vitro cytotoxicity of new pyrrolopyrimidine derivatives is reported in this work. All the compounds were characterized by IR, NMR and MS. They are examined for cytotoxic activity against HeLa. Pyrrolopyrimidine derivatives of benzyl amine (8g) and 4-bromoaniline (8k) showed a potent activity, which is comparable to that of standard Sorafenib.

scholarly journals The cytotoxic activity of pine needles ethanolic extract of Pinus merkusii on HeLa cell lines

2021 ◽  
Vol 33 ◽  
pp. 03001
Author(s):  
Annise Proboningrat ◽  
Amaq Fadholly ◽  
Sri Agus Sudjarwo ◽  
Fedik Abdul Rantam ◽  
Agung Budianto Achmad
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Ethanolic Extract ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Cytotoxicity Assessment ◽  
Pinus Merkusii

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.

scholarly journals Synthesis and In vitro cytotoxic activity evaluation of (E)-16-(substituted benzylidene) derivatives of dehydroepiandrosterone

2013 ◽  
Vol 21 (1) ◽  
Author(s):  
Mohsen Vosooghi ◽  
Hoda Yahyavi ◽  
Kouros Divsalar ◽  
Hashem Shamsa ◽  
Asma Kheirollahi ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Activity Evaluation ◽  
Derivatives Of

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Syntheses and PDT activity of new mono- and di-conjugated derivatives of chlorin e6

2017 ◽  
Vol 21 (04-06) ◽  
pp. 354-363 ◽  
Author(s):  
Hui Chen ◽  
Stewart W. Humble ◽  
R. G. Waruna Jinadasa ◽  
Zehua Zhou ◽  
Alex L. Nguyen ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Chlorin E6 ◽  
New Compounds ◽  
Derivatives Of

Syntheses of three new chlorin e6 conjugates for PDT of tumors are reported. One of the new compounds 17 is conjugated with lysine at the 131-position, but the others are mono-conjugated 14 or diconjugated 15 with the non-amino acid species ethanolamine. Cellular experiments with the three new compounds and previously synthesized non-amino acid 152-conjugates (7–10), 131-monoconjugates 14, 16, and a 131,152-diconjugate 12 are reported. In vitro cytotoxicity experiments show that the 131-conjugates are more toxic than the 152-conjugates, and the most toxic derivative (dark- and photo-toxicity) is the 131-ethylenediamine conjugate 11. The most useful PDT photosentitizers appear to be the ethanolamine derivatives, conjugated at the 152- and the 131,152-positions; these show high phototoxicity but relatively low dark toxicity compared with 11, and also the highest dark/photo cytotoxicity ratios.

scholarly journals Synthesis and cytotoxicity of 3-amino-glycyrrhetinic acid derivatives

2018 ◽  
Vol 7 (1) ◽  
pp. 39-55 ◽  
Author(s):  
Martin Sahn ◽  
Anja Grupe ◽  
Lucie Heller ◽  
Hidayat Hussain ◽  
Ahmed Al-Harrasi ◽  
...  
Keyword(s):  
Parent Compound ◽  
Human Tumor ◽  
In Vitro Cytotoxicity ◽  
Glycyrrhetinic Acid ◽  
Human Tumor Cell Lines ◽  
Amino Esters ◽  
Cytotoxic Compound ◽  
Amino Derivatives ◽  
Derivatives Of

The aim of this study was to prepare 3-hydroximino- and 3-amino derivatives of glycyrrhetinic acid and derivatives to evaluate their in vitro cytotoxicity for a panel of human tumor cell lines. Thus, commercially available glycyrrhetinic acid (1) was acetylated or oxidized at position C-3 and transformed into a variety of different esters and amides followed by their conversion to 3-oximes and amines. While the parent compound was not cytotoxic at all, the 3-amino esters are highly cytotoxic. Interestingly, 3-amino amides were significantly less cytotoxic than 3-amino esters. The (3b, 18b, 20b) Benzyl 3-amino-11-oxoolean-12-en-30-oate was the most cytotoxic compound of this series showing an EC50 = 1.3 mM for 518A2 melanoma cells.

Synthesis of α-Aminoalkyl Phosphonate Derivatives of Resveratrol as Potential Antitumour Agents

2008 ◽  
Vol 61 (6) ◽  
pp. 472 ◽  
Author(s):  
Lei Shi ◽  
Xian-Feng Huang ◽  
Zhen-Wei Zhu ◽  
Huan-Qiu Li ◽  
Jia-Yu Xue ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Tumour Cell Line ◽  
Partial Synthesis ◽  
Antitumour Agents ◽  
Inhibition Concentration ◽  
Ic50 Values ◽  
Epidermoid Tumour ◽  
Derivatives Of

Several α-aminoalkyl phosphonate derivatives of resveratrol were first prepared by partial synthesis from resveratrol. Antitumour activities of the synthesized compounds were determined against a human nasopharyngeal epidermoid tumour cell line KB and a human normal cell line L02 in vitro. The results indicated that these compounds showed good cytotoxic activity against KB but weak cytotoxic activity against L02. Compounds 5c and 5d showed significant cytotoxic activity against KB, with median inhibition concentration (IC50) values of 0.4 μM and 0.9 μM, respectively. On the basis of the biological results, the structure–activity relationship is discussed concisely. The potent antitumour activities shown by 5c and 5d make these resveratrol phosphonate derivatives of great interest for further investigations.

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