75105-02-1Relevant academic research and scientific papers
Thiazole containing nitrogen mustards: Synthesis, structural evaluation, cytotoxicity and DNA binding studies
Raghavendra, Nulgulmnalli Manjunathiah,Renuka, Surampudi,Gupta, Sayan Dutta,Divya, Pingili
, p. 838 - 842 (2011)
The present anticancer research demands more potent anticancer agents with fewer side effects than the existing ones. A series of novel substituted thiazole and benzothiazole containing nitrogen mustards (5-8; 15-17; 22-23) were synthesized and the structures of the compounds were analyzed by IR, NMR and mass spectras. Their in-vitro cytotoxicity against human lung carcinoma (A549) was investigated by MTT Assay. The compounds 16, 8 showed promising activity against A549 human lung carcinoma cell lines with % CPI 52 (More than Cisplatin) and 45.9 respectively. The DNA binding properties of the compounds were also evaluated based on their affinity or intercalation with CT-DNA measured with absorption titration. The compounds 22 and 5 showed the highest binding affinity with binding constant (Ki) 48.34 and 41.8 respectively.
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities as σ1 receptor ligands
Ferorelli, Savina,Abate, Carmen,Pedone, Maria P.,Colabufo, Nicola A.,Contino, Marialessandra,Perrone, Roberto,Berardi, Francesco
experimental part, p. 7612 - 7622 (2012/01/04)
Starting from two carbocyclic analogs, a series of 3,3-dimethylpiperidine derivatives was prepared and tested in radioligand binding assays at σ1 and σ2 receptors, and at Δ8-Δ7 sterol isomerase (SI) site. The novel compounds mostly bear heterocyclic rings or bicyclic nucleus of differing lipophilicities. Compounds 18a and 19a,b demonstrated the highest σ1 affinity (Ki = 0.14-0.38 nM) with a good selectivity versus σ2 binding. Among them, 18a had the lowest C log D value (3.01) and only 19b was selective versus SI too. Generally, it was observed that more planar and hydrophilic heteronuclei conferred a decrease in affinity for both σ receptor subtypes.
Unexpected reactivity of annulated 3H-benzothiazol-2-ylideneamines as an acyl transfer catalyst
Kobayashi, Megumi,Okamoto, Sentaro
, p. 4347 - 4350 (2007/10/03)
Catalytic ability of annulated 3H-benzothiazol-2-ylideneamines and 1H-pyridin-2-ylideneamines for acylation of alcohols was investigated and 3,4-dihydro-2H-9-thia-1,4a-diazafluorene (2b) was found to be an extremely effective catalyst, the reaction with which was faster than that with DMAP.
