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1081“…A series of steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone were designed and prepared by a convenient heterocyclization reaction. …”
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1082por Lee, Sang Jae, Han, Byeong-Gu, Cho, Jea-Won, Choi, Jang-Sik, Lee, Jaekyoo, Song, Ho-Juhn, Koh, Jong Sung, Lee, Byung IlEnlace del recurso
Publicado 2018
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1083por Bharate, Jaideep B., McConnell, Nicholas, Naresh, Gunaganti, Zhang, Lingtian, Lakkaniga, Naga Rajiv, Ding, Lucky, Shah, Neil P., Frett, Brendan, Li, Hong-yu“…We report herein the discovery and therapeutic evaluation of 4,6-diamino pyrimidine-based Type-II FLT3 inhibitors, which can serve as a FLT3-selective scaffold for further clinical development.…”
Publicado 2018
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1084por Dudzinska, Wioleta, Suska, M., Lubkowska, A., Jakubowska, K., Olszewska, M., Safranow, K., Chlubek, D.“…This indicates the possibility of performing high-intensity work with a lower loss of not only purine but also pyrimidine.…”
Publicado 2017
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1085“…To explore the SAR of this structural prototype, twenty-four novel N(2),N(4)-disubstituted pyrimidine-2,4-diamines were designed and synthesized. …”
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1086“…Using as a precursor for the synthesis of new pyrazolo pyrimidine derivatives 9–10. The major incentive behind the preparation of these compounds was the immense biological activities associated to these heterocyclic derivatives. …”
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1087“…PURPOSE: The objective of this study was to describe the direct new method for preparation of novel pyrazolo[1,5-a]pyrimidine derivatives and their corresponding cycloalkane ring-fused derivatives. …”
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1088por Lawrence, Karl P., Douki, Thierry, Sarkany, Robert P. E., Acker, Stephanie, Herzog, Bernd, Young, Antony R.“…We demonstrate photodamage in this region for a number of different endpoints including cell viability, DNA damage (delayed cyclobutane pyrimidine dimers), differential gene expression (for genes associated with inflammation, oxidative stress and photoageing) and induction of oxidizing species in vitro in HaCaT keratinocytes and in vivo in human volunteers. …”
Publicado 2018
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1089por Lough, Lea, Sherman, Dan, Becerra-Flores, Manuel, Vasudevan, Deepika, Lavinda, Olga, Ni, Eric, Wang, Hong, Ryoo, Hyung Don, Tibes, Raoul, Cardozo, Timothy“…We synthesized and evaluated a series of GCN2 inhibitors based on a triazolo[4,5-d]pyrimidine scaffold. Several compounds potently inhibited GCN2 in vitro and displayed good selectivity over the related kinases PERK, HRI, and IRE1. …”
Publicado 2018
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1090por Yang, Chao-Fu, Gopula, Balraj, Liang, Jian-Jong, Li, Jin-Kun, Chen, Si-Yu, Lee, Yi-Ling, Chen, Ching S., Lin, Yi-Ling“…As DHODH is a key enzyme in the de novo pyrimidine biosynthesis pathway, these AR-12 derivatives may act by targeting pyrimidine biosynthesis in host cells to inhibit viral replication. …”
Publicado 2018
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1091por He, Hai-Yun, Zhao, Jin-Ni, Jia, Ruo, Zhao, Ying-Lan, Yang, Sheng-Yong, Yu, Luo-Ting, Yang, Li“…In a cell-based screen of novel anticancer agents, the hit compound 1a which bears a pyrazolo[3,4-d]pyrimidine scaffold exhibited high inhibitory activity against a panel of four different types of tumor cell lines. …”
Publicado 2011
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1092por Yang, Tao, He, Hong, Ang, Wei, Yang, Ying-Hong, Yang, Jian-Zhong, Lin, Yan-Ni, Yang, Hua-Cheng, Pi, Wei-Yi, Li, Zi-Cheng, Zhao, Ying-Lan, Luo, You-Fu, Wei, Yuquan“…A series of N-3-substituted 7-aminopyrido[2,3-d]pyrimidin-6-carbonitrile derivatives was readily synthesized and their anti-proliferative activities on five types of tumor cells were evaluated through a cell-based phenotypic screening approach. …”
Publicado 2012
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1093por Farghaly, Thoraya A., Abbas, Eman M. H., Dawood, Kamal M., El-Naggar, Tarek B. A.“…Two series of naphtho[1,8-ef][1,4]diazepines and pyrrolo[1,2-a]perimidines were prepared starting from 1,8-diaminonaphthalene and hydrazonoyl chlorides. …”
Publicado 2014
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1094“…A novel one pot synthesis of pyrazolo[4′,3′:5,6]pyrido[2,3-d]pyrimidine-diones, via a five-component reaction, involving, hydrazine hydrate, ethyl acetoacetate, and 1,3-dimethyl barbituric acid, an appropriate aryl aldehydes and ammonium acetate catalyzed via both of heterogeneous and homogeneous catalysis in water, is reported.…”
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1095por Helma, Robert, Bažantová, Pavla, Petr, Marek, Adámik, Matej, Renčiuk, Daniel, Tichý, Vlastimil, Pastuchová, Alena, Soldánová, Zuzana, Pečinka, Petr, Bowater, Richard P., Fojta, Miroslav, Brázdová, Marie“…We demonstrate that p53 binds to all studied non-B DNA structures, with a preference for non-B DNA structures formed by pyrimidine (Py) rich strands. Using deletion mutants, we determined the C-terminal DNA binding domain of p53 to be crucial for recognition of such non-B DNA structures. …”
Publicado 2019
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1096“…[Image: see text] 2-(2-Bromovinyl)benzimidazoles and 2-(2-bromophenyl)benzimidazoles react with cyanamide by microwave irradiation in dimethylformamide in the presence of a catalytic amount of CuI along with a base to give the corresponding benzo[4,5]imidazo[1,2-c]pyrimidin-1-amines and benzo[4,5]imidazo[1,2-c]quinazolin-6-amines, respectively, in moderate to good yields. 2-(2-Bromophenyl)indoles also react with cyanamide under similar conditions to afford indolo[1,2-c]quinazolin-6-amines. …”
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1097por Li, Zhonghua, Ding, Lina, Li, Zhongrui, Wang, Zhizheng, Suo, Fengzhi, Shen, Dandan, Zhao, Taoqian, Sun, Xudong, Wang, Junwei, Liu, Ying, Ma, Liying, Zhao, Bing, Geng, Pengfei, Yu, Bin, Zheng, Yichao, Liu, Hongmin“…The findings further indicate that targeting LSD1 is a promising strategy for AML treatment, the triazole-fused pyrimidine derivatives are new scaffolds for the development of LSD1/KDM1A inhibitors.…”
Publicado 2019
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1098por Sirakanyan, Samvel N., Spinelli, Domenico, Geronikaki, Athina, Hakobyan, Elmira K., Sahakyan, Harutyun, Arabyan, Erik, Zakaryan, Hovakim, Nersesyan, Lusine E., Aharonyan, Anahit S., Danielyan, Irina S., Muradyan, Rafayel E., Hovakimyan, Anush A.“…Continuing our research in the field of new heterocyclic compounds, herein we report on the synthesis and antitumor activity of new amino derivatives of pyrido[3′,2′:4,5](furo)thieno[3,2-d]pyrimidines as well as of two new heterocyclic systems: furo[2–e]imidazo[1,2-c]pyrimidine and furo[2,3-e]pyrimido[1,2-c]pyrimidine. …”
Publicado 2019
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1099por Peytam, Fariba, Adib, Mehdi, Shourgeshty, Reihaneh, Firoozpour, Loghman, Rahmanian-Jazi, Mahmoud, Jahani, Mehdi, Moghimi, Setareh, Divsalar, Kouros, Faramarzi, Mohammad Ali, Mojtabavi, Somayeh, Safari, Fatemeh, Mahdavi, Mohammad, Foroumadi, Alireza“…In an attempt to find novel α-glucosidase inhibitors, an efficient, straightforward reaction to synthesize a library of fully substituted 6-amino-pyrazolo[1,5-a]pyrimidines 3 has been investigated. Heating a mixture of α-azidochalcones 1 and 3-aminopyrazoles 2 under the mild condition afforded desired compounds with a large substrate scope in good to excellent yields. …”
Publicado 2020
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1100por Casalvieri, Kimberly A., Matheson, Christopher J., Backos, Donald S., Reigan, Philip“…The data have been obtained for a series of substituted pteridinones and pyrimidines that were developed based on BI-D1870 to establish a structure-activity relationship for RSK inhibition. …”
Publicado 2020
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