Pd(PPh3)4 Catalyzed Synthesis of Indazole Derivatives as Potent Anticancer Drug

Jagan Mohana Rao Saketi,S N Murthy Boddapati,Hari Babu Bollikolla,Syed Farooq Adil,Osamah Alduhaish,Mohammed Rafiq H Siddiqui,Raghuram M,Mohammed Rafi Shaik

doi:10.3390/app10113792

Jagan Mohana Rao Saketi, S N Murthy Boddapati + Show 6 more

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https://doi.org/10.3390/app10113792

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Abstract

A series of 3-aryl indazoles and 1-methyl-3-aryl indazole derivatives are prepared with exceptional yields by coupling with several arylboronic acids and methylation by two dissimilar approaches. The as-prepared indazole derivatives (3a–3j) and their N-methyl derivatives (5a–5j) are evaluated for in vitro anticancer activity against two cancer cell lines, HCT-116 and MDA-MB-231. The results reveal that the indazole derivatives tested display mild to moderate anticancer activities against the cell lines tested.

Highlights

Cancer, a disease of the cell cycles, has remained the largest cause of mortality and morbidity for several decades
Inspired by the above facts, and in continuation of our efforts towards the development of new heterocyclic moieties of therapeutic importance [44,45,46], in the present investigation, we report the synthesis of a series of 3-aryl-1H- indazoles and N-methyl-3-arylindazoles using Pd(PPh3 )4 catalyst methodologies towards the construction of various heterocyclic compounds using Cu catalyst
The solvent from the reaction mixture was evaporated; the crude solid obtained was dissolved in ethyl acetate and washed with water and brine, dried over sodium sulfate and the solvent removed under vacuum to give a crude compound N-methyl-3-aryl indazole

Summary

Introduction

A disease of the cell cycles, has remained the largest cause of mortality and morbidity for several decades now. In spite of rapid development in diagnostic and therapeutic protocols, according to the World Health Organization (WHO), cancer holds second place after cardiovascular disease as a cause of death in the world [1]. Among all the available therapeutic methods, chemotherapy still remains a significant option for the treatment of cancer, which has emerged as a new era of molecularly targeted therapeutics [2]. The development of novel, potent, and selective anticancer agents is still one of the most significant areas of modern cancer research and turns out to be the main objective of organic and medicinal chemists across the world

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