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|---|---|---|---|
| 001 | 660129 | ||
| 005 | 20231030041654.0 | ||
| 035 | _a(RuTPU)RU\TPU\network\29079 | ||
| 090 | _a660129 | ||
| 100 | _a20190426a2018 k y0engy50 ba | ||
| 101 | 0 | _aeng | |
| 102 | _aUS | ||
| 135 | _adrcn ---uucaa | ||
| 181 | 0 | _ai | |
| 182 | 0 | _ab | |
| 200 | 1 |
_aSynthesis, biochemical evaluation and computational simulations of new cytochrome bc1 complex inhibitors based on N-(4-aryloxyphenyl) phthalimides _vElectronic resource _fCheng Hua [et al.] |
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| 203 |
_aText _celectronic |
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| 300 | _aTitle screen | ||
| 320 | _a[References: 57 tit.] | ||
| 330 | _aThe cytochrome bc1 complex (the bc1 complex or complex III) is an attractive target for the discovery of numerous pharmaceuticals and pesticides. In order to identify new lead structures for this target, a new series of molecules, N-(4-aryloxyphenyl)phthalimides, were designed and synthesized in a straightforward manner. Our design strategy was to introduce a 4-aryloxyphenyl group, a fragment which exhibited promising bc1 complex-inhibiting properties, into the aryl group of the valuable N-arylphthalimide backbone. Afterward, the biochemical evaluation of the newly synthesized compounds was carried out, and the results implied that several compounds demonstrated good activities against succinate-cytochrome reductase (SCR, a mixture of mitochondrial complex II and the bc1 complex). Further studies confirmed that 3e', a representative compound in this paper, was identified as an inhibitor of the bc1 complex. Furthermore, computational simulations were also performed to better understand binding of 3e' to the enzyme complex, which indicated that 3e' should bind to the Qo site of the bc1 complex. Consequently, we harbor the idea that this paper can provide a solid platform for synthesis and discovery of other bc1 complex inhibitors. | ||
| 333 | _aРежим доступа: по договору с организацией-держателем ресурса | ||
| 461 | _tChinese Chemical Letters | ||
| 463 |
_tVol. 29, iss. 12 _v[P. 1897-1900] _d2018 |
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| 610 | 1 | _aэлектронный ресурс | |
| 610 | 1 | _aтруды учёных ТПУ | |
| 610 | 1 | _acytochrome bc1 complex | |
| 610 | 1 | _ainhibitor | |
| 610 | 1 | _asynthesis | |
| 610 | 1 | _abiochemical evaluation | |
| 610 | 1 | _acomputational simulation | |
| 610 | 1 | _aцитохром | |
| 610 | 1 | _aингибиторы | |
| 610 | 1 | _aсинтез | |
| 610 | 1 | _aбиохимические показатели | |
| 610 | 1 | _aкомпьютерное моделирование | |
| 701 | 0 | _aCheng Hua | |
| 701 | 0 | _aFu Yan | |
| 701 | 0 | _aChang Qing | |
| 701 | 0 | _aZhang Ni | |
| 701 | 0 | _aBu Mengwei | |
| 701 | 0 | _aNiu Yan | |
| 701 | 0 | _aWu Qiongyou | |
| 701 | 0 | _aChen Cheng | |
| 701 | 1 |
_aVerpoort _bF. V. K. _cChemical Engineer _cProfessor of Tomsk Polytechnic University, doctor of chemical Sciences _f1963- _gFrensis Valter Kornelius _2stltpush _3(RuTPU)RU\TPU\pers\35059 |
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| 712 | 0 | 2 |
_aНациональный исследовательский Томский политехнический университет _bИсследовательская школа химических и биомедицинских технологий (ИШХБМТ) _c(2017- ) _h8120 _2stltpush _3(RuTPU)RU\TPU\col\23537 |
| 801 | 2 |
_aRU _b63413507 _c20190426 _gRCR |
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| 856 | 4 | _uhttps://doi.org/10.1016/j.cclet.2018.10.008 | |
| 942 | _cCF | ||