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Literature DB >> 7277388

Novel immunosuppressive agents. Potent immunological activity of some bensothiopyrano [4,3-c]pyrazol-3-ones.

Abstract

A unique class of immunosuppressive agents has been found be the use of a mouse model of immunity. A number of bensothiopyrano[4,3-c]pyrazol-3-ones are potent inhibitors of both the humoral and cellular immune response developed in mice in response to El4 tumor cells. These compounds exhibit a selectivity for inhibiting the humoral response. Structure-activity relationships and Hansch analyses of data from the mouse model are discussed. One of the most potent compounds, 2-(4'-chlorophenyl)bensothiopyrano[4,3-c]pyrazol-3-one (1, CP-17 193), exhibits ED50 values for inhibiting the humoral and cellular responses in the range of 0.5-2 mg/kg, po, in the mouse model and also inhibits antibody production to several other antigens and prolongs skin graft survival in mice. These compounds are shown in several ways to be distinct from the lymphocytotoxic drugs cyclophosphamide and azathioprine.

Entities: Chemical Disease Species

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Year: 1981 PMID： 7277388 DOI： 10.1021/jm00139a012

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

10 in total

1. Cinchona alkaloid catalyzed enantioselective amination of α,β-unsaturated ketones: an asymmetric approach to Δ²-pyrazolines.

Authors: Nathaniel R Campbell; Bingfeng Sun; Ravi P Singh; Li Deng
Journal: Adv Synth Catal Date: 2011-11-01 Impact factor: 5.837

2. Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents.

Authors: Hanumappa Ananda; Kothanahally S Sharath Kumar; Mayilaadumveettil Nishana; Mahesh Hegde; Mrinal Srivastava; Raghava Byregowda; Bibha Choudhary; Sathees C Raghavan; Kanchugarakoppal S Rangappa
Journal: Mol Cell Biochem Date: 2016-11-24 Impact factor: 3.396

3. The effects of CP 17193, an immunosuppressive pyrazaloquinoline, on the development of spontaneous lupus disease in NZBW F1 hybrid mice.

Authors: R V Bundick; R P Eady
Journal: Clin Exp Immunol Date: 1992-08 Impact factor: 4.330

4. 1-[5-(4-Meth-oxy-phen-yl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl]ethanone.

Authors: Asghar Abbas; Safdar Hussain; Noureen Hafeez; Kong Mun Lo; Aurangzeb Hasan
Journal: Acta Crystallogr Sect E Struct Rep Online Date: 2010-11-13

5. A trisubstituted pyrazole derivative reduces DMBA-induced mammary tumor growth in rats by inhibiting estrogen receptor-α expression.

Authors: Hanumappa Ananda; Kothanahally S Sharath Kumar; Muddenahalli S Sudhanva; Shobith Rangappa; Kanchugarakoppal S Rangappa
Journal: Mol Cell Biochem Date: 2018-05-18 Impact factor: 3.396

10. Utility of 5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide in the synthesis of heterocyclic compounds with antimicrobial activity.

Authors: Abdou O Abdelhamid; Ibrahim E El Sayed; Yasser H Zaki; Ahmed M Hussein; Mangoud M Mangoud; Mona A Hosny
Journal: BMC Chem Date: 2019-04-01

10 in total

Novel immunosuppressive agents. Potent immunological activity of some bensothiopyrano [4,3-c]pyrazol-3-ones.

1. Cinchona alkaloid catalyzed enantioselective amination of α,β-unsaturated ketones: an asymmetric approach to Δ²-pyrazolines.

2. Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents.

3. The effects of CP 17193, an immunosuppressive pyrazaloquinoline, on the development of spontaneous lupus disease in NZBW F1 hybrid mice.

4. 1-[5-(4-Meth-oxy-phen-yl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl]ethanone.

5. A trisubstituted pyrazole derivative reduces DMBA-induced mammary tumor growth in rats by inhibiting estrogen receptor-α expression.

6. Comparative activity of CP-17,193 and five established immunosuppressives toward the antigens SRBC and EL4.

7. 1-[3-(2-Nitro-phen-yl)-5-phenyl-2-pyrazolin-1-yl]ethanone.

8. 1-Acetyl-3-(4-chloro-phen-yl)-5-(4-fluoro-phen-yl)-2-pyrazoline.

9. 5-Benzoyl-N,4-diphenyl-4,5-dihydro-1H-pyrazole-3-carboxamide.

10. Utility of 5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide in the synthesis of heterocyclic compounds with antimicrobial activity.