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Synthesis and Antitumour Activity of 1 H ,3 H ‐Thiazolo[3,4‐ a ]benzimidazole Derivatives
Author(s) -
Chimirri Alba,
Monforte Pietro,
Musumeci Laura,
Rao Angela,
Zappalà Maria,
Monforte AnnaMaria
Publication year - 2001
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/1521-4184(200106)334:6<203::aid-ardp203>3.0.co;2-l
Subject(s) - benzimidazole , cell culture , chemistry , in vitro , selectivity , stereochemistry , biological activity , chemical synthesis , cell growth , growth inhibition , cancer cell lines , structure–activity relationship , combinatorial chemistry , cancer cell , biochemistry , cancer , biology , organic chemistry , genetics , catalysis
A series of 1 H ,3 H ‐thiazolo[3,4‐ a ]benzimidazoles were synthesized and tested for their in vitro antitumour activity against 60 human tumour cell lines. Some derivatives exhibited both tumour growth inhibition activity and cellular selectivity. In particular, compound 8c , the most active of the series, was very active towards all cell lines at concentrations ranging from 10 −7 −10 −5 M. Compound 4a , on the other hand, was highly selective against the CNS cancer cell line.