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Indazole, an important fused aromatic heterocyclic system containing benzene and pyrazole ring with a chemical formula of C<jats:sub>7<\/jats:sub>H<jats:sub>6<\/jats:sub>N<jats:sub>2<\/jats:sub>, is also called benzopyrazole. Indazoles consist of three tautomeric forms in which 1<jats:italic>H<\/jats:italic>\u2010tautomers (indazoles) and 2<jats:italic>H<\/jats:italic>\u2010tautomers (isoindazoles) exist in all phases. The tautomerism in indazoles greatly influences synthesis, reactivity, physical and even the biological properties of indazoles. The thermodynamic internal energy calculation of these tautomers points view 1<jats:italic>H<\/jats:italic>\u2010indazole as the predominant and stable form over 2<jats:italic>H<\/jats:italic>\u2010indazole. The natural source of indazole is limited and exists in alkaloidal nature (i.e., nigellidine, nigeglanine, nigellicine, etc.) found from <jats:italic>Nigella<\/jats:italic> plants. Some of the FDA\u2010approved drugs like Axitinib, Entrectinib, Niraparib, Benzydamine, and Granisetron are being used to treat renal cell cancer, non\u2010small cell lung cancer (NSCLC), epithelial ovarian cancer, chronic inflammation, chemotherapy\u2010induced nausea, vomiting, and many more uses. Besides all these advantages regarding its biological activity, the main issue about indazoles is the less abundance in plant sources, and their synthetic derivatives also often face problems with low yield. In this review article, we discuss its chemistry, tautomerism along with their effects, different schematics for the synthesis of indazole derivatives, and their different biological activities.<\/jats:p>","DOI":"10.1002\/ddr.21979","type":"journal-article","created":{"date-parts":[[2022,8,16]],"date-time":"2022-08-16T05:42:23Z","timestamp":1660628543000},"page":"1469-1504","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":77,"title":["A review on synthetic strategy, molecular pharmacology of indazole derivatives, and their future perspective"],"prefix":"10.1002","volume":"83","author":[{"given":"Suvadeep","family":"Mal","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Siksha 'O' Anusandhan University (Deemed to be University) Bhubaneswar Odisha India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Udita","family":"Malik","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Guru Ghasidas Vishwavidyalaya (A Central University) Bilaspur Chhattisgarh India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Monalisa","family":"Mahapatra","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Siksha 'O' Anusandhan University (Deemed to be University) Bhubaneswar Odisha India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Abhishek","family":"Mishra","sequence":"additional","affiliation":[{"name":"Aurobindo Pharma Morrisville, Durham North Carolina USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dilipkumar","family":"Pal","sequence":"additional","affiliation":[{"name":"Department of Pharmacy Guru Ghasidas Vishwavidyalaya (A Central University) Bilaspur Chhattisgarh India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1210-2293","authenticated-orcid":false,"given":"Sudhir K.","family":"Paidesetty","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Siksha 'O' Anusandhan University (Deemed to be University) Bhubaneswar Odisha India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,8,16]]},"reference":[{"key":"e_1_2_14_2_1","first-page":"313","article-title":"Synthesis and biological activities of a novel series of indazole derivatives","volume":"5","author":"Aanandhi M. 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