Design, Synthesis, and Evaluation of Bis‐Benzothiazole Derivatives as DNA Minor Groove Binding Agents

A series of novel bis‐benzothiazole derivatives with head‐to‐head orientation were designed, synthesized, and evaluated for their anti‐proliferative activities on U937, HL60, and HeLa cells. A significant part of the targets exhibited considerable in vitro anticancer activity, and some of them were...

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Published inJournal of heterocyclic chemistry Vol. 55; no. 1; pp. 360 - 365
Main Authors Yang, Ming‐Li, Zhang, Huan, Wang, Wei‐Wei, Wang, Xiu‐Jun
Format Journal Article
LanguageEnglish
Published HOBOKEN Wiley 01.01.2018
Wiley Subscription Services, Inc
Subjects
Anticancer properties
Chemistry
Chemistry, Organic
Deoxyribonucleic acid
Derivatives
DNA
Fluorescence
Physical Sciences
Science & Technology
ISATIN
IN-VITRO
UPDATE
ANTITUMOR-ACTIVITY
ANTI-TUBERCULAR ACTIVITY
HYBRIDS
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Summary:A series of novel bis‐benzothiazole derivatives with head‐to‐head orientation were designed, synthesized, and evaluated for their anti‐proliferative activities on U937, HL60, and HeLa cells. A significant part of the targets exhibited considerable in vitro anticancer activity, and some of them were more potent than the reference 5‐FU. Molecular modeling, fluorescence, and viscosimetry studies revealed that these compounds could bind into the minor groove of DNA. Amongst them, the most active compound 7 with IC50 in a range of 6.76 to 8.67 μM against the tested three cell lines, which was 1.46–2.47 and 3.48–4.93 times more potent than 5‐FU and Hoechst 33258, respectively, warrant further investigations.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.3041