Pharmaceutical Sciences and Natural Products - Research Publications

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    Hetero Cyclic Compounds in the Treatment of Triple-Negative Breast Cancer
    (Bentham Science Publishers, 2023-01-02T00:00:00) Mandal, Sudip Kumar; Das, Agnidipta; Bose, Anindya; Dwibedi, Vagish; Ganguly, Paramita; Sarkar, Sipra; Prakash, Ranjana; Dey, Biplab Kumar; Mandal, Sanjeet; Rath, Santosh Kumar
    Triple-negative breast cancer (TNBC) holds just about 15% of all breast tumours and sub-types of breast cancer with distinct characteristics of negative expressions for the progesterone recep-tor, estrogen receptor, and human epidermal growth factor receptor 2. Unfortunately, treatment options for TNBCs are minimal. Most currently available therapies proved inefficient in holding back this aggressive natural treatment of TNBC, in most cases calling for an immediate need for more effective and safer anti-TNBC agents. Based on research reported in recent years, this review pre-sents the report's overview of anti-TNBC compounds and their efficacy, being classified according to the structures. Breast Cancer type 1 and type 2 genes (BRCA1/2) mutations are associated with TNBC. Poly (ADP-Ribose) Polymerases (PARPs) are a family of enzymes involved in numerous cellular processes, including DNA repair. PARP-1 inhibition is involved in the loss of DNA repair via BRCA-dependent mechanisms. PARP-1 inhibitors like Olaparib, Rucaparib, Niraparib, and Tala-zoparib have proved as promising therapeutic medications as monotherapy and in combination with cytotoxic therapy or radiotherapy in various types of cancers. This review is focused on presenting the status of therapeutics against TNBC. The critical spotlight of this review is to encapsulate the versatility and notable success of heterocyclic pharmacophores-based molecules in treating TNBC. � 2023 Bentham Science Publishers.
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    A comprehensive review on bioactive fused heterocycles as purine-utilizing enzymes inhibitors
    (Birkhauser Boston, 2015) Chauhan, Monika; Kumar, Raj
    Purine-utilizing enzymes (PUEs) are involved in the control of biological actions of nitrogen-containing bases, purines and pyrimidines, by participating in their catabolism, and this has made them a topic of considerate interest. The heterocyclics, as purine-utilizing enzyme inhibitors (PUEIs), play a vital role in a number of diseases, e.g., malaria, cancer, rheumatoid arthritis, inflammation, tissue rejection, and autoimmune disorders. The present review is first of its kind covering the literature up to 2014 on the advances in broad-spectrum medicinal activities exhibited by heterocycles as PUEIs. The drug designing of the purine and pyrimidine antimetabolites is based on the structural mimicking of the existing compounds. The basic consideration during the designing of this class is the introduction of small structural changes without the alteration of basic skeleton of pharmacophore. The balance between the existing empirical approach and rational approach is yet to be maintained during the design and synthesis of new PUEIs by combining in vivo, in vitro, and in silico methods. The data compiled in the present manuscript on SARs, IC50s, Kis, Km, in silico studies, and their reported X-ray co-crystal structures with PUEs will offer the researchers the rational approaches for the design and development of selective and specific PUEIs devoid of adverse effects. ? 2014 Springer Science+Business Media.