Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

A series of novel diethylene glycol tethered isatin‐1,2,3‐triazole‐coumarin hybrids 9a–l were designed, synthesized, and evaluated for their in vitro anticancer activities against HepG2 (liver carcinoma), Hela (cervical cancer), A549 (lung adenocarcinoma), DU145 (prostatic cancer), SKOV3 (ovarian carcinoma), MCF‐7 (breast cancer), and drug‐resistant MCF‐7/DOX (doxorubicin‐resistant MCF‐7) human cancer cell lines. The results showed that most of the synthesized hybrids exhibited considerable in vitro activities against the tested seven cancer cell lines, and these hybrids can be acted as starting points for further investigation.

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and In Vitro Anticancer Activities of Diethylene Glycol Tethered Isatin‐1,2,3‐triazole‐coumarin Hybrids

Quan-ping

Guo

Wang

2019

“…Among heterocyclic compounds, isatin‐based, 1,2,3‐triazole‐based, and coumarin‐based compounds have broad biological activity spectrum including antitubercular , antibacterial , antiviral , antimalarial , and anticancer properties. Moreover, some of them such as sunitinib, carboxyamidotriazole, and STX64 (Fig.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Evaluation of Tetraethylene Glycol‐Tethered Isatin–1,2,3‐Triazole–Coumarin Hybrids as Novel Anticancer Agents

Zhao

et al. 2019

We report herein the design and synthesis of a series of novel tetraethylene glycol‐tethered isatin–1,2,3‐triazole–coumarin hybrids and evaluate their in vitro antitumor activities against seven common human cancer cell lines including drug‐resistant cell line. Results revealed that all the synthesized hybrids showed weak to moderate activities against the tested seven cancer cell lines. The structure–activity relationship was also discussed, and the enriched structure–activity relationship may pave the way for further rationale design of this kind of hybrids.

“…Isatin and triazole derivatives possess diverse biological and pharmacological properties such as antitubercular , antibacterial , antiviral , antimalarial , and anticancer activities, occupying an important position in the drug discovery. Several isatin‐ or triazole‐based compounds such as sunitinib, nintedanib, semaxanib, and carboxyamidotriazole (Fig.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Antitumor Activities of 1,2,3‐triazole‐diethylene Glycol Tethered Isatin Dimers

Fan

Huang

Liu

2018

A series of novel 1,2,3‐triazole‐diethylene glycol tethered isatin dimers were designed, synthesized, and screened for their in vitro antitumor activities in this paper. All dimers showed promising activities against the tested HepG2, Hela, A549, DU145, SKOV3, MCF‐7, and doxorubicin‐resistant MCF‐7 human cancer cell lines. The most active dimer 7g was >1.55 folds more potent than etoposide against all tested cell lines, warrant further investigation.