NDLI: Synthesis and cytotoxic studies of some novel compounds containing 3-(1H-indol-3-yl)-1H-pyrazole molecular scaffold

Content Provider	Springer Nature Link
Author	Zhang, Datong Xu, Rongrong Guo, Shoudong Zhu, Yaling
Copyright Year	2014
Abstract	In our efforts to develop effective treatment agents for cancer, a series of novel compounds based on 3-(1H-indol-3-yl)-1H-pyrazole scaffold and three common pharmacophores, namely thiazolidine, 1,3,4-oxadiazole, and acylpyrazole, were synthesized and evaluated for their cytotoxic activity against four human cancer cell lines. Among compounds 2a–2c and 3a–3c containing thiazolidine moiety, 2b and 3c showed moderate cytotoxic activity toward Ho-8910. The dramatic enhancement in cytotoxic activity was observed upon the introduction of a 1,3,4-oxadiazole-2-thiol moiety on 3-(1H-indol-3-yl)-1H-pyrazole scaffold. Compound 5a was the most effective against KG-1 with IC$_{50}$ = 6.09 μM, which was comparable to the reference drug doxorubicin. Compound 5b was potent against HepG-2 (IC$_{50}$ = 9.39 μM) and Ho-8910 (IC$_{50}$ = 9.41 μM). Compound 5e exhibited IC$_{50}$ value of 14.12 μM against A-549 and was more potent than other compounds in this series. Compound 5b induced the highest population of apoptotic cells (28.18 %) among the tested compounds at 10 μM. The results obtained from compounds 5 warrant their further optimization as new leads for developing new anticancer agents.
Starting Page	6575
Ending Page	6587
Page Count	13
File Format	PDF
ISSN	09226168
Journal	Research on Chemical Intermediates
Volume Number	41
Issue Number	9
e-ISSN	15685675
Language	English
Publisher	Springer Netherlands
Publisher Date	2014-09-21
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	3-(1H-indol-3-yl)-1H-pyrazole Thiazolidine 1,3,4-Oxadiazole Acylpyrazole Synthesis Cytotoxic activity Apoptosis Catalysis Physical Chemistry Inorganic Chemistry
Content Type	Text
Resource Type	Article
Subject	Chemistry

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