- Design, synthesis, in vitro antiproliferative evaluation and in silico studies of new VEGFR-2 inhibitors based on 4-piperazinylquinolin-2(1H)-one scaffold
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Angiogenesis is essential in the growth of solid tumors which need oxygen and nutrients supply to grow in size. The VEGF/VEGFR-2 signaling pathway plays an important role in tumor angiogenesis. Sorafenib is an FDA approved cancer therapeutic with activity
- Abdelhamid, Dalia,Abourehab, Mohammed A. S.,Abuo‐Rahma, Gamal El‐Din A.,Badr, Mohamed,Hassan, Abdelfattah,Hassan, Heba A.
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- Regioselective synthesis of 2-chloroquinoline based ethyl 4-(3-hydroxyphenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates and their In-Silico evaluation against P. Falciparum lactate dehydrogenase
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The reaction of various substituted 2, 4-dichloroquinolines with ethyl 4-(3-hydroxyphenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate was carried out in the presence of K2CO3 as a mild and efficient base at controlled temperature leading to novel 2-chloroquinoline based polyhydroquinoline with high regioselectivity. All the synthesized compounds were characterized using IR, NMR, Mass spectral data and then subjected to an in-silico analysis against P. falciparum lactate dehydrogenase.
- Rajesh, Kancherla,Lavanya, Pandian,Iniyavan, Pethaperumal,Sarveswari, Sundaramoorthy,Ramaiah, Sudha,Anbarasu, Anand,Vijayakumar, Vijayaparthasarathi
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p. 789 - 797
(2015/12/01)
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- 4-Aminoquinolone piperidine amides: Noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity
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4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequencing of mutants raised against AQs, identified decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) as the primary target responsible for the antitubercular activity. Mass spectrometry and enzyme kinetic studies indicated that AQs are noncovalent, reversible inhibitors of DprE1 with slow on rates and long residence times of ~100 min on the enzyme. In general, AQs have excellent leadlike properties and good in vitro secondary pharmacology profile. Although the scaffold started off as a single active compound with moderate potency from the whole cell screen, structure-activity relationship optimization of the scaffold led to compounds with potent DprE1 inhibition (IC50 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb.
- Naik, Maruti,Humnabadkar, Vaishali,Tantry, Subramanyam J.,Panda, Manoranjan,Narayan, Ashwini,Guptha, Supreeth,Panduga, Vijender,Manjrekar, Praveena,Jena, Lalit Kumar,Koushik, Krishna,Shanbhag, Gajanan,Jatheendranath, Sandesh,Manjunatha,Gorai, Gopinath,Bathula, Chandramohan,Rudrapatna, Suresh,Achar, Vijayashree,Sharma, Sreevalli,Ambady, Anisha,Hegde, Naina,Mahadevaswamy, Jyothi,Kaur, Parvinder,Sambandamurthy, Vasan K.,Awasthy, Disha,Narayan, Chandan,Ravishankar, Sudha,Madhavapeddi, Prashanti,Reddy, Jitendar,Prabhakar,Saralaya, Ramanatha,Chatterji, Monalisa,Whiteaker, James,McLaughlin, Bob,Chiarelli, Laurent R.,Riccardi, Giovanna,Pasca, Maria Rosalia,Binda, Claudia,Neres, Jo?o,Dhar, Neeraj,Signorino-Gelo, Fran?ois,McKinney, John D.,Ramachandran, Vasanthi,Shandil, Radha,Tommasi, Ruben,Iyer, Pravin S.,Narayanan, Shridhar,Hosagrahara, Vinayak,Kavanagh, Stefan,Dinesh, Neela,Ghorpade, Sandeep R.
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supporting information
p. 5419 - 5434
(2014/07/08)
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- Regioselective synthesis of novel 2-chloroquinoline derivatives of 1,4-dihydropyridines
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Highly regioselective reaction of some substituted 2,4-dichloroquinolines with symmetrical 1,4-dihydropyridines, leading to novel quinoline derivatives of DHPs, has been achieved in the presence of powdered K2CO 3, as a mild and efficient base, at moderate temperature. All the synthesized compounds were characterized by use of IR, NMR, and mass spectral data.
- Rajesh,Iniyavan,Sarveswari,Vijayakumar
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p. 1851 - 1866
(2014/05/06)
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- THERAPEUTIC AGENTS I
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Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
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Page/Page column 39
(2010/02/12)
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