SYNTHESIS OF 2-ARYL INDAZOLE: SYNTHESIS, BIOLOGICAL EVALUATION AND IN-SILICO STUDIES

Vamshi Krishna Atikala; Siddique Akber Ansari; Irfan Aamer Ansari; Ravikumar Kapavarapu; Hari Babu Bollikolla

doi:10.1002/cbdv.202302085

SYNTHESIS OF 2-ARYL INDAZOLE: SYNTHESIS, BIOLOGICAL EVALUATION AND IN-SILICO STUDIES

Chem Biodivers. 2024 Apr 26:e202302085. doi: 10.1002/cbdv.202302085. Online ahead of print.

Authors

Vamshi Krishna Atikala¹, Siddique Akber Ansari², Irfan Aamer Ansari³, Ravikumar Kapavarapu⁴, Hari Babu Bollikolla⁵

Affiliations

¹ Acharya Nagarjuna University, chemistry, nnagar, 522510, guntur, INDIA.
² King Saud University, chemistry, Riyadh, 11451, riyadh, SAUDI ARABIA.
³ University of Turin, chemistry, Turin, 10124, turin, ITALY.
⁴ Nirmala College of Pharmacy, Pharmacy, Atmakur, Mangalagiri Mandal, 522502, Mangalagiri, INDIA.
⁵ Acharya Nagarjuna University, chemistry, guntur, 522510, India, 522510, GUNTUR, INDIA.

PMID: 38666662
DOI: 10.1002/cbdv.202302085

Abstract

In this work, a highly effective synthesis technique for obtaining aryl indazole under mild circumstances is provided, using trimethyl phosphine as a powerful reagent. The procedure shows that a wide range of substrates can be investigated, yielding various 2-aryl indazole derivatives with acceptable to exceptional yields and a wide range of functional group tolerance. Additionally, based on In Silico studies tests were conducted to determine the anticancer activity In Vitro for all produced compounds (3a-3j) against A549, HT-29 and HepG2 cell lines. Compounds 3c and 3d, with IC50 values of 15, 53.55, 7.34, 7.10, 56.28, and 17.87 (µM) against A549, HT-29 and HepG2 respectively, showed significant anticancer activity.

Keywords: 2-Nitro benzaldehyde; 2-aryl indazoles; Anticancer activity; Primary amines; Trimethyl phosphine.