Design, Synthesis, and Anticancer Evaluation of Tetrazole-Fused Benzoxazole Derivatives as Tubulin Binding Agents


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Аннотация

A novel series of tetrazole fused benzoxazole derivatives 9a9j are synthesized, and their structures are characterized by 1H and 13C NMR, and mass spectra. The compounds 9a, 9b, 9g, 9h, and 9j demonstrate the highest activity. The compounds 9b and 9g exhibit good anticancer activity, in particular against MCF7, Hop62, and A-549 cell lines with the range of GI50 values from <0.1 to 4.56 μM. Molecular docking study is carried out for the compounds 9a9j, according to which the compound 9b forms one hydrogen bond with THR766 with the highest docking score (–7.33). This indicates that 9b is effeciently binging to tubulin site.

Авторлар туралы

P. Ravikumar

Department of Chemistry; GVK Biosciences Private Limited, Nacharam, IDA Mallapur

Хат алмасуға жауапты Автор.
Email: ravipolothi@gmail.com
Үндістан, Hyderabad, Telangana, 500082; Hyderabad, Telangana, 500076

G. Raolji

GVK Biosciences Private Limited, Nacharam, IDA Mallapur

Email: ravipolothi@gmail.com
Үндістан, Hyderabad, Telangana, 500076

K. Venkata Sastry

CMR College of Pharmacy, Medchal

Email: ravipolothi@gmail.com
Үндістан, Hyderabad, Telangana, 501401

S. Kalidasu

Department of Chemistry; GVK Biosciences Private Limited, Nacharam, IDA Mallapur

Email: ravipolothi@gmail.com
Үндістан, Hyderabad, Telangana, 500082; Hyderabad, Telangana, 500076

T. Balaaraju

Department of Chemistry, School of Science

Email: ravipolothi@gmail.com
Үндістан, Hyderabad, Telangana, 502329

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© Pleiades Publishing, Ltd., 2018