- Development of novel rhodanine analogs as anticancer agents: Design, synthesis, evaluation and comsia study
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Background: A series of novel 5-substituted benzylidene rhodanine derivatives using four different amines were designed based on our previously developed CoMSIA (Comparative molecular similarity indices analysis) model for the anticancer activity. Method:
- Krithika, Uma,Prabitha,Mandal, Subhankar P.,Yuvaraj,Priya,Wadhwani, Ashish D.,Prashantha Kumar
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p. 216 - 229
(2021/03/03)
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- NOVEL COMPOUND AS MTOR INHIBITOR AND USE THEREOF
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The present invention relates to a novel compound as an mTOR inhibitor and a use thereof and, more specifically, to a novel compound represented by formula 1 that exhibits mTOR inhibitory activity and a pharmaceutical composition comprising same as an act
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Paragraph 0063; 0095
(2021/03/04)
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- Synthesis and Antitumor Activity of New 5-Ylidene Derivatives of 3-(Furan-2-ylmethyl)-2-sulfanylidene-1,3-thiazolidin-4-one
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Abstract: Reactions of 3-(furan-2-ylmethyl)-2-sulfanyidene-1,3-thiazolidin-4-one with aromatic and heterocyclic aldehydes afforded a series of previously unknown 5-[(het)arylmethylidene]-3-(furan-2-ylmethyl)-2-sulfanylidene-1,3-thiazolidin-4-ones. Treatment of 3-(furan-2-ylmethyl)-2-sulfanylidene-1,3-thiazolidin-4-one with thionyl chloride gave in a good yield 3,3′-bis(furan-2-ylmethyl)-2,2′-disulfanylidene-5,5′-bi-1,3-thiazolidinylidene-4,4′-dione which was reduced with zinc in acetic acid to 3,3′-bis(furan-2-ylmethyl)-2,2′-disulfanylidene-5,5′-bi-1,3-thiazolidine-4,4′-dione. The synthesized compounds were screened for antitumor activity.
- Horishny, V. Ya.,Matiychuk, V. S.
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p. 1600 - 1605
(2020/10/22)
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- A concise approach to n-substituted rhodanines through a base-assisted one-pot coupling and cyclization process
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An efficient approach to obtain functionalized rhodanines was developed through a base-assisted one-pot coupling and continuous cyclization of a primary amine, carbon disulfide, and methyl (2-chloroacetyl)carbamate. This conversion tolerates a broad range of functional groups and can be used to scale the preparation of N-substituted rhodanines in excellent yields.
- Huo, Zhipeng,Liang, Yongxi,Sun, Xun,Tang, Mei-Lin,Zhang, Chenchen
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- A facile synthesis of novel 3-(aryl/alkyl-2-ylmethyl)-2-thioxothiazolidin- 4-ones using microwave heating
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(Z)-5-(2-(1H-Indol-3-yl)-2-oxoethylidene)-3-(aryl/alkyl-2-ylmethyl) -2-thioxothiazolidin-4-ones (7a-w) have been synthesized by the Knoevenagel condensation reaction of 3-(aryl/alkyl-2-ylmethyl)-2-thioxothiazolidin-4-ones (3a-d) with suitably substituted 2-(1H-indol-3-yl)2-oxoacetaldehydes (6a-g) under microwave conditions. The thioxothiazolidin-4-ones were prepared from the corresponding aryl/alkyl amines (1a-d) and di-(carboxymethyl)-trithiocarbonyl (2). The aldehydes (6a-g) were synthesized from the corresponding acid chlorides (5a-g) using HsnBu3.
- Kamila, Sukanta,Ankati, Haribabu,Harry, Emily,Biehl, Edward R.
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supporting information; experimental part
p. 2195 - 2198
(2012/05/20)
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- Electrogenerated base-promoted synthesis of N-benzylic rhodanine and carbamodithioate derivatives
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Electrogenerated magnesium-associated cyanomethyl anions/bases obtained from the electrochemical reduction of acetonitrile and the oxidation of a sacrificial magnesium rod were successfully used to promote the addition of carbon disulfide to primary benzylic amines. Alkylation with ethyl 3-bromopropionate acid ester or with ethyl 2-bromoacetate acid ester yields the corresponding ring-opened carbamodithioate compounds or cyclic rhodanine derivatives, respectively. The effect of the amount of electrogenerated base on the yield of reaction was also evaluated.
- Tissaoui, Khalil,Raouafi, Noureddine,Boujlel, Khaled
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experimental part
p. 41 - 48
(2010/10/03)
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- REACTION OF CHLOROACETYL CHLORIDE WITH THE SALTS OF N-ALKYL(ARYL)DITHIOCARBAMIC ACIDS - A CONVENIENT METHOD FOR THE SYNTHESIS OF 3-SUBSTITUTED RHODANINES
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Rhodanine and its 3-substituted derivatives are readily obtained in the reaction of monochloroacetyl chloride with the ammonium salts of N-substituted dithiocarbamic acids.A possible reaction mechanism, involving S -> N-acyl migration, is discussed.
- Krus, K.,Masias, A.,Beletskaya, I. P.
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p. 1824 - 1825
(2007/10/02)
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