Journal of Medicinal Chemistry

, том 59 , издание 16 , страницы 7677-7682

1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists

Idrees Mohammed ¹

Indrasena Reddy Kummetha ²

Gatikrushna Singh ¹

Natalia Sharova ³

Gianluigi Lichinchi ^{1, 2}

Jason Dang ²

Mario Stevenson ³

Tariq Rana ^{1, 2}

Скрыть аффилиации авторов Показать аффилиации авторов: 3 аффилиации

Program for RNA Biology, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, California 92037, United States |

Department of Pediatrics, University of California San Diego School of Medicine, 9500 Gilman Drive, MC 0762, La Jolla, California 92093 United States |

Division of Infectious Diseases, Miller School of Medicine, University of Miami, Miami, Florida 33136, United States |

Тип публикации: Journal Article

Дата публикации: 2016-08-10

American Chemical Society (ACS)

Journal of Medicinal Chemistry

scimago Q1

wos Q1

БС1

SJR: 1.801

CiteScore: 11.5

Impact factor: 6.8

ISSN: 00222623, 15204804

DOI: 10.1021/acs.jmedchem.6b00247

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PubMed ID: 27509004

Drug Discovery

Molecular Medicine

Краткое описание

RN-18 based viral infectivity factor (Vif), Vif antagonists reduce viral infectivity by rescuing APOBEC3G (A3G) expression and enhancing A3G-dependent Vif degradation. Replacement of amide functionality in RN-18 (IC50 = 6 μM) by isosteric heterocycles resulted in the discovery of a 1,2,3-trizole, 1d (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a 1d based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μM).

Найдено

2 цитирования

Беляев Евгений

🤝

к.х.н.

34 публикации, 223 цитирования

Индекс Хирша: 10

Институт физической химии и электрохимии им. А.Н. Фрумкина РАН

2 цитирования

Цветков Владимир

🤝

PhD

88 публикаций, 1 272 цитирования, 1 рецензия

Индекс Хирша: 19

Институт нефтехимического синтеза им. А.В. Топчиева РАН

Первый Московский государственный медицинский университет имени И. М. Сеченова

Федеральный научно-клинический центр физико-химической медицины имени академика Ю.М. Лопухина ФМБА

Области научных интересов

Drug design

Materials Chemistry

Modelling and Simulations

Компьютерное моделирование

квадруплексы и i-мотивы ДНК и РНК

2 цитирования

Ларина Людмила

56 публикаций, 361 цитирование, 2 рецензии

Индекс Хирша: 10

Иркутский институт химии им. А.Е. Фаворского СО РАН

Центр Фотохимии

Институт биохимической физики им. Н.М. Эмануэля РАН

Национальный университет Чунгнам

1 цитирование

Тихонов Андрей

7 публикаций, 55 цитирований

Индекс Хирша: 3

Первый Московский государственный медицинский университет имени И. М. Сеченова

Российский Университет Дружбы Народов

Области научных интересов

Адресная доставка лекарств

Молекулярная биология

Молекулярная генетика

Редактирование генома

1 цитирование

Скворцова Юлия

23 публикации, 272 цитирования

Индекс Хирша: 10

Институт биоорганической химии им. академиков М.М. Шемякина и Ю.А. Овчинникова РАН

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Mohammed I. et al. 1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists // Journal of Medicinal Chemistry. 2016. Vol. 59. No. 16. pp. 7677-7682.

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Mohammed I., Kummetha I. R., Singh G., Sharova N., Lichinchi G., Dang J., Stevenson M., Rana T. 1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists // Journal of Medicinal Chemistry. 2016. Vol. 59. No. 16. pp. 7677-7682.

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TY - JOUR

DO - 10.1021/acs.jmedchem.6b00247

UR - https://doi.org/10.1021/acs.jmedchem.6b00247

TI - 1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists

T2 - Journal of Medicinal Chemistry

AU - Mohammed, Idrees

AU - Kummetha, Indrasena Reddy

AU - Singh, Gatikrushna

AU - Sharova, Natalia

AU - Lichinchi, Gianluigi

AU - Dang, Jason

AU - Stevenson, Mario

AU - Rana, Tariq

PY - 2016

DA - 2016/08/10

PB - American Chemical Society (ACS)

SP - 7677-7682

IS - 16

VL - 59

PMID - 27509004

SN - 0022-2623

SN - 1520-4804

ER -

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@article{2016_Mohammed,

author = {Idrees Mohammed and Indrasena Reddy Kummetha and Gatikrushna Singh and Natalia Sharova and Gianluigi Lichinchi and Jason Dang and Mario Stevenson and Tariq Rana},

title = {1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists},

journal = {Journal of Medicinal Chemistry},

year = {2016},

volume = {59},

publisher = {American Chemical Society (ACS)},

month = {aug},

url = {https://doi.org/10.1021/acs.jmedchem.6b00247},

number = {16},

pages = {7677--7682},

doi = {10.1021/acs.jmedchem.6b00247}

}

MLA

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MLA Скопировать

Mohammed, Idrees, et al. “1,2,3-Triazoles as Amide Bioisosteres: Discovery of a New Class of Potent HIV-1 Vif Antagonists.” Journal of Medicinal Chemistry, vol. 59, no. 16, Aug. 2016, pp. 7677-7682. https://doi.org/10.1021/acs.jmedchem.6b00247.

Издатель

American Chemical Society (ACS)

Журнал

Journal of Medicinal Chemistry

scimago Q1

wos Q1

БС1

SJR

1.801

CiteScore

11.5

Impact factor

6.8

ISSN

00222623 (Print)

15204804 (Electronic)