Synthesis and biological evaluation of designed molecules
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Scopus Publications
Scopus Publications
A Comprehensive Review of Designing and Synthetic Aspects of Pyrazolopyrimidine Derivatives as Anticancer Agents Preet Sagar, Yogita Sachin Ozarde, Vijaya Sachin Vichare, Preeti Prashant Mehta, Ranjit Vinayak Gadhave Mini Reviews in Medicinal Chemistry, 2026 Background: Pyrazolopyrimidines are a fascinating class of heterocyclic compounds that have attracted considerable interest for their potential in cancer therapy. Their unique scaffold allows flexible chemical modifications, enabling them to interact with various cancer-related proteins— especially kinases that regulate tumor growth and survival. Objective: This review highlights recent advancements in the design, synthesis, and biological evaluation of pyrazolopyrimidine derivatives, emphasizing their role as targeted anticancer agents. Methods: We analyzed recent literature (2000–2025) covering synthetic strategies, anticancer targets, in silico studies on anticancer targets and their mechanisms, off-target mechanisms, and patent information. The review also focuses on how these methods guide the optimization of Structure– Activity Relationships (SAR) and improve compound efficacy. Results: Numerous pyrazolopyrimidine derivatives demonstrated significant anticancer activity across various cell lines, including breast, liver, colorectal, and haematological malignancies. Mechanistic investigations revealed that these derivatives target key oncogenic pathways, such as CDKs, EGFR (including resistant mutants), mTOR, TOPO II, and HDACs. They exert anticancer effects by inducing apoptosis, arresting cells at S or M phases, and downregulating proliferation markers. Several studies also report favourable selectivity for cancer cells, improved bioavailability, and metabolic stability, supporting their drug-like properties. Conclusion: Pyrazolopyrimidines represent a versatile and promising class with strong in vivo efficacy, selectivity, and a favorable toxicity profile. Their ability to engage multiple targets and overcome resistance highlights their potential for integration in oncology. However, further systematic in vivo and clinical studies are essential to translate their potential into therapeutic success.
DESIGN, SYNTHESIS AND EVALUATION OF N-(BENZO[D]THIAZOL-2-YL)-2-OXO-2H-CHROMENE-3-CARBOXAMIDE DERIVATIVES AS POTENTIAL ANTIOXIDANT AND ANTIBACTERIAL AGENTS Ranjit V. Gadhave, , Sachin S. Khade, Yogita S. Ozarde, Somdatta Y. Chaudhari, Arti G. Swami, Mukesh K. Meena Indian Drugs, 2022 This research is focused on designing, synthesis and biological evaluation of a series of coumarin based benzothiazole derivatives. The ligands were identified by docking study for antioxidant and antibacterial potential using target proteins PDB:4H1J and PDB:3G75, respectively. The target molecules were synthesized as a series of substituted N-(benzothiazol-2-yl)-2-oxo-chromene-3-carboxamides (7a–h) by condensation of substituted benzo[d]thiazol-2-amines with in situ synthesized substituted 2-oxo-2H-chromene-3-carbonyl chlorides. Infrared spectroscopy and 1 H- nuclear magnetic resonance spectra were used to characterize the synthesized molecules. In vitro antioxidant activity of compounds was evaluated by DPPH and H2 O2 radical scavenging assays. Antibacterial potential of compounds was evaluated using well diffusion method against Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922) and Pseudomonas aeruginosa (ATCC 27853). Among synthesized derivatives, 7a showed good antioxidant potential whereas 7f showed antibacterial activity, which might be employed as lead molecules for future investigation for respective activities.
Design, synthesis, characterization and antioxidant activity of novel benzothiazole and coumarin based 6-(3, 5-dimethylpyrazol-1-yl) pyridazin-3-one derivatives Ranjit V. Gadhave, Bhanudas S. Kuchekar Research Journal of Pharmacy and Technology, 2020 The present work describes biological evaluation of target molecules designed by molecular docking with 4h1j protein using Autodock Vina docker. Designed novel benzothiazole and coumarin based 6-(3, 5-dimethylpyrazol-1-yl) pyridazin-3-one derivatives were synthesized by condensation of substituted 6-(3,5-dimethylpyrazol-1-yl)pyridazin-3(2H)-one with substituted 2-amino benzothiazoles, substituted 2-oxo-2H-chromene-3-carbonyl chloride or 4-(bromomethyl)-2H-chromen-2-one. Synthesized compounds were characterized by spectral analysis and screened for antioxidant activity using 1, 1-diphenyl-2-picrylhyrazyl radical scavenging, Hydrogen peroxide scavenging and ferric reducing antioxidant power method. The compounds 5c and 9b showed more antioxidant potential and other compounds showed moderate to less activity as compared to standard Ascorbic acid and Butylated hydroxyl toluene.
Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives Ranjit V. Gadhave, Bhanudas S. Kuchekar Asian Journal of Chemistry, 2020 A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.
Design, synthesis, characterization and biological evaluation of novel benzothiazole based [1, 2, 4]-triazolo [4, 3-A] quinoxaline derivatives Indian Drugs, 2019
Stability indicating RP-HPLC-PDA method for determination of abiraterone acetate and characterization of its base catalyzed degradation product by LC-MS International Journal of Pharmacy and Pharmaceutical Sciences, 2016
