A. Santillán | Semantic Scholar

Publications
Influence

Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis.

L. Gomez, M. Hack, T. K. Jones
Chemistry
Bioorganic & medicinal chemistry letters
15 May 2007

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Inhibitors of the glycine transporter type-2 (GlyT-2): synthesis and biological activity of benzoylpiperidine derivatives.

R. Wolin, A. Santillán, L. Tang, Charles Q. Huang, Xiaoxia Jiang, T. Lovenberg
Chemistry, Biology
Bioorganic & medicinal chemistry
15 August 2004

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Novel glycine transporter type-2 reuptake inhibitors. Part 2: beta- and gamma-amino acid derivatives.

R. Wolin, A. Santillán, T. Lovenberg
Chemistry, Biology
Bioorganic & medicinal chemistry
2004

Several beta- and gamma-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [(14)C]-glycine in COS7 cells transfected with human glycine…

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Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains.

John J. M. Wiener, L. Gomez, Cheryl A. Grice
Biology, Chemistry
Bioorganic & medicinal chemistry letters
15 May 2007

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Critical Role of the Linking Amide in CC-1065 and the Duocarmycins: Implications on the Source of DNA Alkylation Catalysis

D. Boger, A. Santillán, M. Searcey, Qing Jin
Chemistry, Biology
3 November 1998

The preparation and evaluation of both enantiomers of 5 are described and it constitutes an analogue of CBI-TMI (4), the duocarmycins, and CC-1065 in which the amide linking the alkylation and DNA methylation is linked to the TMI molecule.

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Role of the [4.2.2] Bicyclic Unit in Bicyclomycin: Synthesis, Structure, Chemical, Biochemical, and Biological Properties.

A. Santillán, Hyeung-geun Park Hg, Xiangdong Zhang, O. Lee, W. Widger, H. Kohn
Chemistry, Biology
The Journal of organic chemistry
1 November 1996

Findings indicated that the [4.2.2] bicyclic unit played an important role in the antibiotic-rho recognition process and placement of an irreversible inactivating unit at the N- and O-sites within the [3.3.4] ring system would likely prohibit the bicyclomycin derivative from efficiently binding to rho.

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Synthesis and evaluation of 1,2,8, 8a-Tetrahydrocyclopropa[c]pyrrolo[3,2-e]indol-4(5H)-one, the parent alkylation subunit of CC-1065 and the duocarmycins: impact of the alkylation subunit…

D. Boger, A. Santillán, Q. Jin
Chemistry
The Journal of organic chemistry
10 May 2000

Establishment of the DNA binding properties revealed that the CPI-based agents retain the identical DNA alkylation selectivities of the natural products.

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C(5)-C(5a)-modified bicyclomycins: synthesis, structure, and biochemical and biological properties.

F. Vincent, J. Srinivasan, A. Santillán, W. Widger, H. Kohn
Chemistry, Biology
The Journal of organic chemistry
6 April 2001

It is found that extending the C(5)-C(5a) double bond with unsaturated substituents provides bicyclomycin derivatives with excellent inhibitory activities in the biochemical assay, and that enhanced inhibitory activity is observed for the C (5E) geometrical isomer compared with its C( 5Z) counterpart.

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Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.

W. Eccles, J. Blevitt, Arlene L Young
Chemistry
Bioorganic & medicinal chemistry letters
1 February 2013

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Role of the C(6)-hydroxy group in bicyclomycin: synthesis, structure, and chemical, biochemical, and biological properties.

A. Santillán, X. Zhang, J. Hardesty, W. Widger, H. Kohn
Chemistry, Biology
Journal of medicinal chemistry
26 March 1998

It is found that replacing the C(6)-hydroxy group in 1 with weaker hydrogen bond donors led to low inhibitory activities in the rho-dependent ATPase and transcription termination assays, and none of the bicyclomycin derivatives exhibited antibiotic activity against E. coli.

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