Steroidal 5α-Reductase Inhibitors: A Comparative 3D-QSAR Study Review

Thareja, Suresh

doi:10.1021/cr5005953

Cited by 24 publications

(12 citation statements)

References 96 publications

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“…. The net charge distributions of aryl fluoride and thiophene Grignard reagent were computed using MOPAC2012 with a minimum energy conformation of its molecular structure (the Hamiltonian approximation Austin model 1 (AM1) was used for the minimized structures in order to achieve the lowest energy structures) . The results are outlined in Fig.…”

Section: Resultsmentioning

confidence: 99%

Nickel‐catalysed Kumada polycondensation of di‐functionalized Grignard reagent with aryl fluoride

Han

Zong

Liu

et al. 2016

Polymer International

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A nickel catalyst promoted the polymerization between various Grignard reagents with 2-phenyl-4,6-bi(4-fluorophenyl)-1,3,5triazine. The reaction scope was thoroughly investigated and fully characterized. The Sp 2 -C − F bond was successfully activated by the triazine group in Kumada coupling reactions. Also, di-Grignard reagents showed higher activity than mono-Grignard reagents. The reaction scope results reveal that a Grignard reagent with strong nucleophilicity and aryl fluoride with strong electrophilicity are necessary to lead to Kumada polycondensation of oligothiophenes with aryl fluoride. In this work, polymerization between di-functionalized oligothiophene Grignard reagents with aryl fluoride was first conducted. The weight-average molecular weight is high, up to 14.8 kDa. The -conjugated polymers obtained exhibit emission colours of blue, green and yellow with efficient photoluminescence.

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Section: Resultsmentioning

confidence: 99%

Nickel‐catalysed Kumada polycondensation of di‐functionalized Grignard reagent with aryl fluoride

Han

Zong

Liu

et al. 2016

Polymer International

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“…It has been shown that the double bond between positions C4 and C5 on the steroidal ring A, confers a negative cytotoxic effect on cancer cells for 3-hydroxyimino-substituted compounds [35]. This suggests that antiproliferative activity may also be mediated, at least to some extent, by a different behavior between steroidal oximes 4 and 5 , related to the conformational difference on the rings A/B (a double bond shift) and it is possible that compound 4 may be recognized more easily by the active site in the cell by binding to protein- associated signaling molecules [73]. From this information our future work will focus on the search for new routes to synthesize steroidal derivatives with oxime moieties on a larger scale and on the search for molecular mechanisms involved in antiproliferative activity.…”

Section: Discussionmentioning

confidence: 99%

Antiproliferative, Cytotoxic, and Apoptotic Activity of Steroidal Oximes in Cervicouterine Cell Lines

et al. 2016

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Abstract:Steroidal sapogenins have shown antiproliferative effects against several tumor cell lines; and their effects on human cancer cells are currently under study. Changes in the functionality on the steroidal structure make it possible to modify the biological activity of compounds. Herein, we report the synthesis and in vitro antitumor activity of two steroidal oxime compounds on cervical cancer cells. These derivatives were synthesized from the steroidal sapogenin diosgenin in good yields. The in vitro assays show that the steroidal oximes show significant antiproliferative activity compared to the one observed for diosgenin. Cell proliferation, cell death, and the cytotoxic effects were determined in both cervical cancer cells and human lymphocytes. The cancer cells showed apoptotic morphology and an increased presence of active caspase-3, providing the notion of a death pathway in the cell. Significantly, the steroidal oximes did not exert a cytotoxic effect on lymphocytes.

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“…1,2 Inhibitors of T2-5-reductase, such as the clinically used drug finasteride, are potentially useful for the treatment of benign prostate hyperplasia. 3,4 The 3-arylmethylidene pyrrolidine-2,5-dione exo-1ae has been investigated with regard to its vasorelaxant activity, which was reported to be in the range of the standard drug doxazosin. 5 Compounds of the general formula exo-1 have been used as Michael acceptors for irreversible, site-specific thiol bioconjugation, 6 as test substrates for asymmetric transformations, [7][8][9] and as starting materials to access other heterocyclic systems, such as pyrolo quinolines 10 or coumarins.…”

Section: Table Of Contents Graphicmentioning

confidence: 99%

Iterative Arylation of Itaconimides with Diazonium Salts through Electrophilic Palladium Catalysis: Divergent β-H-Elimination Pathways in Repetitive Matsuda–Heck Reactions

et al. 2019

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Steroidal 5α-Reductase Inhibitors: A Comparative 3D-QSAR Study Review

Cited by 24 publications

References 96 publications

Nickel‐catalysed Kumada polycondensation of di‐functionalized Grignard reagent with aryl fluoride

Nickel‐catalysed Kumada polycondensation of di‐functionalized Grignard reagent with aryl fluoride

Antiproliferative, Cytotoxic, and Apoptotic Activity of Steroidal Oximes in Cervicouterine Cell Lines

Iterative Arylation of Itaconimides with Diazonium Salts through Electrophilic Palladium Catalysis: Divergent β-H-Elimination Pathways in Repetitive Matsuda–Heck Reactions

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