- AN IMPROVED PROCESS FOR THE PREPARATION OF 4-OXOISOTRETINOIN
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The present invention relates to an improved process for the preparation of 4-Oxoisotretinoin and purification process of 4-Oxoisotretinoin (I) and crystalline 5 form of 4-Oxoisotretinoin (I).
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- Preparation method of olefine acid impurity
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The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of an olefine acid impurity. The impurity is (13E) -3, 7-dimethyl -9 -[(3RS) -3-methoxy -2, 6, 6-trimethyl cyclohexenyl] -2, 4, 6, 8-azela
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Paragraph 0057-0058
(2021/01/11)
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- 13-CIS-RAMBA RETINAMIDES THAT DEGRADE MNKS FOR TREATING CANCER
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The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induc
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Page/Page column 53
(2016/06/20)
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- Novel C-4 heteroaryl 13- cis -retinamide Mnk/AR degrading agents inhibit cell proliferation and migration and induce apoptosis in human breast and prostate cancer cells and suppress growth of MDA-MB-231 human breast and CWR22Rv1 human prostate tumor xenografts in mice
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The synthesis and in vitro and in vivo antibreast and antiprostate cancers activities of novel C-4 heteroaryl 13-cis-retinamides that modulate Mnk-eIF4E and AR signaling are discussed. Modifications of the C-4 heteroaryl substituents reveal that the 1H-imidazole is essential for high anticancer activity. The most potent compounds against a variety of human breast and prostate cancer (BC/PC) cell lines were compounds 16 (VNHM-1-66), 20 (VNHM-1-81), and 22 (VNHM-1-73). In these cell lines, the compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In PC cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. More importantly, VNHM-1-81 has strong in vivo antibreast and antiprostate cancer activities, while VNHM-1-73 exhibited strong in vivo antibreast cancer activity, with no apparent host toxicity. Clearly, these lead compounds are strong candidates for development for the treatments of human breast and prostate cancers.
- Mbatia, Hannah W.,Ramalingam, Senthilmurugan,Ramamurthy, Vidya P.,Martin, Marlena S.,Kwegyir-Afful, Andrew K.,Njar, Vincent C. O.
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p. 1900 - 1914
(2015/04/27)
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- Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice
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Novel retinoic acid metabolism blocking agents (RAMBAs) have been synthesized and characterized. The synthetic features include introduction of nucleophilic ligands at C-4 of all-trans-retinoic acid (ATRA) and 13-cis-retinoic acid, and modification of ter
- Patel, Jyoti B.,Huynh, Carlic K.,Handratta, Venkatesh D.,Gediya, Lalji K.,Brodie, Angela M. H.,Goloubeva, Olga G.,Clement, Omoshile O.,Nanne, Ivo P.,Soprano, Dianne Robert,Njar, Vincent C. O.
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p. 6716 - 6729
(2007/10/03)
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- A convenient synthesis of retinal derivatives with modified trimethylcyclohexene ring
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A method of simultaneous one-stage synthesis of three retinal derivatives (5,6-dioxo-5,6-seco-, 5,6-dihydro-5,6-epoxy-, and 4-oxoretinal) was proposed, with the yield of the first derivative being ～50%. These compounds are useful tools for studying the an
- Mironova,Leont'eva,Shevyakov,Alexeeva,Shvets,Demina,Krasnokutskaya,Finkel'shtein,Khodonov
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p. 487 - 493
(2007/10/03)
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- Potent inhibition of retinoic acid metabolism enzyme(s) by novel azolyl retinoids
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Novel (±)-4-azolyl retinoic acid analogues 4, 5, 7 and 8 have been designed and synthesized and have been shown to be powerful inhibitors of hamster microsomal all-trans-retinoic acid 4-hydroxylase enzyme(s). (±)-4-(1H-Imidazol-1-yl)retinoic acid (4) is t
- Njar, Vincent C.O.,Nnane, Ivo P.,Brodie, Angela M.H.
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p. 1905 - 1908
(2007/10/03)
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- Specific oxidation of retinoic acid to 4-oxo-retinoic acid in diluted acid solutions
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Treatment of retinoic acid (1a) or its methyl ester (2a) with hydrochloric acid in methanol gave methyl 4-oxo-retinoates (4a - c). Similar oxidation proceeded when 2a was treated with trifluoromethanesulfonic acid in the presence of lithium chloride in methanol.
- Tanaka,Kagechika,Shudo
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p. 356 - 358
(2007/10/02)
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- Cancer Chemopreventive 3-Substituted-4-oxoretinoic Acids
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The introduction of substituents at position 3 of methyl 4-oxoretinoate can be effected in good yields by alkylating the lithium dienolate.A second substituent can be introduced also, but the resulting 3,3-disubstituted-4-oxoretinoates were isolated in lo
- Shealy, Y. Fulmer,Hosmer, Carla A.,Riordan, James M.,Wille, John W.,Rogers, Tina S.,Hill, Donald L.
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p. 3051 - 3056
(2007/10/02)
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- Modification of the intact retinoid structure in the cyclohexenyl region: Alkylation of methyl 4-oxoretinoate
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Alkylation of methyl 4-oxoretinoate under kinetic-control conditions gives predominantly 3-alkyl-4-oxoretinoates. 3,3-Disubstituted 4-oxoretinoates are obtained similarly from the 3-monosubstituted derivatives, although introduction of the second substituent is more difficult. Evidence has been obtained for a much slower rate of alkylation α to the ester group.
- Shealy,Hosmer,Riordan
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p. 1095 - 1098
(2007/10/02)
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