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1.
Appl Biochem Biotechnol ; 194(12): 6438-6467, 2022 Dec.
Article in English | MEDLINE | ID: mdl-35900713

ABSTRACT

Oxygen- and sulphur-based heterocycles form the core structure of many biologically active molecules as well as U.S. FDA-approved drugs. Moreover, they possess broad range of biological activities, viz. anticancer, antiinflammatory, antioxidant, antitumour, antibacterial, antiviral, antidiabetic, anticonvulsant, anti-tubercular, analgesic, anti-leishmanial, antimalarial, antifungal, and anti-histaminic, Hence, O- and S-based heterocycles are gaining more attention in recent years on the road to the discovery of innovative anticancer drugs after the extensive investigation of nitrogen-based heterocycles as anticancer agents. Several attempts have been made to synthesize fused oxygen- and sulphur-based heterocyclic derivatives as joining one heterocyclic moiety with another may lead to improvement in the biological profile of a molecule. Humans have been cursed with cancer since long time. Despite the development of several heterocyclic anticancer medications such as 5-fluorouracil, doxorubicin, methotrexate, and daunorubicin, cure of cancer is difficult. Hence, researchers are trying to synthesize new fused/spiro heterocyclic molecules to discover novel anticancer drugs which may show promising anticancer effects with fewer side effects. Furthermore, fused heterocycles behave as DNA intercalating agents which have the ability to interact with DNA, leading to cell death thereby exerting anticancer effect. This review article highlights the synthesis and anticancer potentiality of oxygen- and sulphur-containing heterocyclic compounds covering the period from 2011 to 2021.


Subject(s)
Antineoplastic Agents , Heterocyclic Compounds , Neoplasms , Humans , Oxygen , Heterocyclic Compounds/pharmacology , Heterocyclic Compounds/therapeutic use , Heterocyclic Compounds/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Antineoplastic Agents/chemistry , Neoplasms/drug therapy , Sulfur
2.
Bioorg Med Chem ; 14(7): 2409-17, 2006 Apr 01.
Article in English | MEDLINE | ID: mdl-16321543

ABSTRACT

A microwave-assisted three-component, regioselective one-pot cyclocondensation method has been developed for the synthesis of a series of novel spiro[indole-thiazolidinones] (6a-l) using an environmentally benign procedure at atmospheric pressure in open vessel. This rapid method produces pure products in high yields within few minutes in comparison to a conventional two-step procedure. The crystal structure of one representative compound has been determined by X-ray diffraction. The synthesized compounds have been screened 'in vitro' for antifungal activity against Rhizoctonia solani, Fusarium oxysporum and Collectotrichum capsici. All compounds have shown good activity against these pathogens.


Subject(s)
Antifungal Agents/chemical synthesis , Benzimidazoles/chemistry , Indoles/chemical synthesis , Spiro Compounds/chemical synthesis , Triazoles/chemistry , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Benzimidazoles/radiation effects , Colletotrichum/classification , Colletotrichum/drug effects , Crystallization , Fusarium/classification , Fusarium/drug effects , Indoles/chemistry , Indoles/pharmacology , Indoles/radiation effects , Microwaves , Models, Molecular , Molecular Structure , Rhizoctonia/classification , Rhizoctonia/drug effects , Spiro Compounds/chemistry , Spiro Compounds/pharmacology , Stereoisomerism , Structure-Activity Relationship , Thiazoles/chemistry , Thiazoles/radiation effects , Thiazolidines , Triazoles/radiation effects , X-Ray Diffraction
3.
Bioorg Med Chem ; 14(5): 1303-8, 2006 Mar 01.
Article in English | MEDLINE | ID: mdl-16242336

ABSTRACT

A facile, dry media procedure has been developed for the synthesis of a series of a new class of fluorine containing 3-alkyl-7-chloro-11a,12-dihydro-11-phenyl-12-(substituted aryl)-11H-benzopyrano[4,3-e][1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazepines (4a-k) under microwaves using basic alumina as solid support. The reaction time has been brought down from hours (60-65 h) to minutes (3-5 min) with improved yield as compared to conventional method, demonstrating the versatility of the process. The method reported herein is devoid of the hazards of solution-phase reactions. The synthesized compounds have been screened 'in vitro' for anti-fungal activity against Rhizoctonia solani, Fusarium oxysporum and Collectotrichum capsici. Most of the compounds have shown good activity against these pathogens.


Subject(s)
Antifungal Agents/pharmacology , Microwaves , Thiazepines/pharmacology , Triazoles/pharmacology , Antifungal Agents/chemical synthesis , Benzopyrans/chemistry , Fluorine/chemistry , Fusarium/drug effects , Microbial Sensitivity Tests , Rhizoctonia/drug effects , Structure-Activity Relationship , Thiazepines/chemical synthesis , Triazoles/chemical synthesis
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