No abstract

In order to explore the anticancer and antimicrobial activity associated with the thiazolone framework, several new (Z)-2-((5-(3fluorobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)carboxylic acid derivatives have been synthesized in water as a solvent. All synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Amongst these, the 3-methylbutanoic and the 3-or 4-methylpentanoic acid derivatives, the 3-hydroxy-, the 3-(1H-imidazol-4-yl) and the 3-(4-hydroxyphenyl)propanoic acid derivatives and the succinic acid derivative showed high antibacterial and antifungal activity. The unsubstituted propanoic acid derivative exhibited significant antibacterial activity against B. subtilis and significant antifungal activity against fungal strains, i.e., A. flavus. The in vitro anticancer studies revealed that the 3-(hydroxy)-, the 3-(1H-imidazol-4yl)-and the 3-(4-hydroxyphenyl)propanoic acid, or the succinic acid derivatives are the most active compounds against MCF-7 and BT-474 human breast cancer cell lines.

In order to explore the anticancer and antimicrobial activity associated with the thiazole framework, we synthesized the new series (Z)‐2‐((5‐(4‐nitrobenzylidene)‐4‐oxo‐4,5‐dihydrothiazol‐2‐yl)amino)‐substituted acid derivatives 6a–l. All the synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Among these, the compounds 6a, 6b, 6c, 6e, 6f, 6g, 6h, 6i, 6j, and 6k showed highest antibacterial and antifungal activity. The compound 6a exhibited significant antibacterial activity against Bacillussubtilis, whereas compound 6j displays significant antifungal activity against fungal strains, that is, A. oryzae. The in vitro anticancer studies revealed that 6e, 6g, 6h, 6k, and 6l are the most active compounds against MCF‐7 and BT‐474 human breast cancer cell lines, which can be regarded as the promising drug candidate for development of anticancer drugs.

Microwave assisted and conventional synthetic methods of new 6-bromo-2-(substituted)-3H-imidazo [4,5-b]pyridine and its derivatives are described, which were obtained in reduced reaction times, higher yields, cleaner reactions than previously described methods. All the synthesized compounds were characterized, and screened for their anticancer and antimicrobial activity. Among synthesized compounds 3b and 3k shows prominent antibacterial activity and compound 3f shows both antibacterial and antifungal activity. Compounds 3h and 3j shows prominent anticancer activity against the both breast cancer cell lines, MCF-7 and BT-474. These results suggest that the imidazo [4,5-b]pyridine moiety may serve as a new promising template for synthesis of anticancer and antimicrobial agents and further study is required for evaluation of their mechanism of action.

No abstract

A highly efficient protocol was developed for the synthesis of 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide compounds with excellent yields. The in vitro anticancer activity of the new 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide derivatives against A549 (lung cancer cell), HeLa (cervical), MCF-7 (breast cancer cell) and Du-145 (prostate cancer cell) cell lines were studied. Most of the tested compounds showed anticancer activity (IC50 values ranged between 1.98 and 9.12 µM against different cell lines).

No abstract

A series of Rhodanine derivatives were synthesized by Knoevenagel condensation. All the synthesized compounds were tested for their in vitro anticancer activity against MCF-7 and BT-474 human breast cancer cell lines. All the synthesized compounds were characterized and screened for their antimicrobial activity against the bacterial and fungal strain. Majority of the compounds showed good to moderate anticancer and antimicrobial activity. Among these compounds, one showed promising activity against gram-positive bacteria B. subtilis and S. aureus when compared with ampicillin. Some of the most potent compounds possessed selective antimicrobial activity.