Eduardo Palomino

Universidad Autónoma de Nuevo León

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Jerome P. Horwitz

Wayne State University

S.C. Brooks

University of Georgia

A. Paul Schaap

LumaMed (United States)

M.J. Heeg

University of Oklahoma

Mary Jane Heeg

Wayne State University

Lisa Polin

The Barbara Ann Karmanos Cancer Institute

Lisa Polin

Wayne State University

A.F.M.M. Rahman

Technische Universität Berlin

Mary Jo Pilat

The Barbara Ann Karmanos Cancer Institute

David Kessel

Wayne State University

Cooperative Institutions

Wayne State University

The Barbara Ann Karmanos Cancer Institute

Wichita State University

Walker Cancer Research Institute

Universidad Autónoma de Nuevo León

University of the West Indies System

Harper University Hospital

University of Michigan–Ann Arbor

University of the West Indies

Michigan United

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Chemical Modulation of Activity in Steroidal Estrogens

CRC Press eBooks (2020)

Eduardo Palomino

This chapter explores the effects that some simple chemical modifications of the basic structure of estradiol can have on estrogenic activity. The attempt is to establish a preliminary basis for structural prediction using molecular modeling, and the consequent correlation with some biological results such as gene induction, as well as the preeminent binding to the estrogen receptor. The correlation of these structures with binding activity and gene induction is poorly understood. However, it should be noted that, although estrogen receptor allows large flexibility in binders, some minimum requirements are essential; thus, minor changes to key molecular areas may have a dramatic effect in estrogen activity. While the repositioning of the hydroxyl group to the C4 location to produce caused very little skeletal change, overall gene induction was turned off despite the fact that receptor binding was better than for isomer. The ultimate goal of these studies is to achieve enough refinement for the theoretical calculation of activity using molecular modeling.

Modulation (music)

10.1201/9781003068754-18

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Citations (1)

Chemical Modulation of Activity in Steroidal Estrogens

Critical Reviews in Biochemistry and Molecular Biology (1999)

Eduardo Palomino

Modulation (music)

10.1080/10409239991209363

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Citations (6)

Identification and antitumor activity of a reduction product in the murine metabolism of pyrazoloacridine (NSC-366140)

Cancer Chemotherapy and Pharmacology (1996)

Eduardo Palomino B J Foster Maya B. Kempff Thomas H. Corbett Richard Wiegand

Metabolic pathway

S9 fraction

Nitro compound

10.1007/s002800050510

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Citations (8)

Photooxygenation of strained epoxides

Tetrahedron Letters (1989)

Eduardo Palomino A. Paul Schaap Mary Jane Heeg

Photooxygenation

Ylide

Ozonide

10.1016/s0040-4039(01)93356-8

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Citations (6)

Implications of receptor binding in the steroid receptor superfamily.

Current opinion in drug discovery & development (1998)

Eduardo Palomino

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Inhibition of breast tumor growth and angiogenesis by a medicinal herb: Ocimum gratissimum

International Journal of Cancer (2007)

Pratima Nangia‐Makker Larry Tait Malathy P.V. Shekhar Eduardo Palomino Victor Hogan

Abstract Ocimum sp. is a traditionally used medicinal herb, which shows anti‐oxidant, anti‐carcinogenic, radio‐protective and free radical scavenging properties. So far no detailed studies have been reported on its effects on human cancers. Thus, we analyzed its effects on human breast cancer utilizing in vitro and in vivo methodologies. Aqueous extracts were prepared from the mature leaves of Ocimum gratissimum (OG) cultivated devoid of pesticides. Tumor progression and angiogenesis related processes like chemotaxis, proliferation, apoptosis, 3D growth and morphogenesis, angiogenesis and tumor growth were studied in the presence or absence of the extract, and in some experiments a comparison was made with purified commercially available eugenol, apigenin and ursolic acid. Aqueous OG leaf extract inhibits proliferation, migration, anchorage independent growth, 3D growth and morphogenesis and induction of COX‐2 protein in breast cancer cells. A comparative analysis with eugenol, apigenin and ursolic acid showed that the inhibitory effects on chemotaxis and 3D morphogenesis of breast cancer cells were specific to OG extract. In addition, OG extracts reduced tumor size and neoangiogenesis in a MCF10 DCIS.com xenograft model of human DCIS. This is the first detailed report showing that OG leaf extract may be of value as a breast cancer preventive and therapeutic agent and might be considered as additional additive in the arsenal of components aimed at combating breast cancer progression and metastasis. © 2007 Wiley‐Liss, Inc.

Ocimum gratissimum

Ursolic acid

10.1002/ijc.22733

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Citations (78)

ChemInform Abstract: Photooxygenation of Strained Epoxides.

ChemInform (1990)

Eduardo Palomino A. Paul Schaap Mary Jane Heeg

Abstract The epoxide (I) is photooxygenated in the presence of 9,10‐dicyanoanthracene to form the cyclic ozonide (II), together with the diketone (III).

Photooxygenation

10.1002/chin.199028079

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Design, Synthesis, and Biological Evaluation of Analogues of the Antitumor Agent, 2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic Acid (XK469)

Journal of Medicinal Chemistry (2001)

Stuart Hazeldine Lisa Polin Juiwanna Kushner Jennifer Paluch Kathryn White

2-{4-[(7-Chloro-2-quinoxalinyl)oxy]phenoxy}propionic acid (XK469) is among the most highly and broadly active antitumor agents to have been evaluated in our laboratories and is currently scheduled to enter clinical trials in 2001. The mechanism or mechanisms of action of XK469 remain to be elaborated. Accordingly, an effort was initiated to establish a pharmacophore hypothesis to delineate the requirements of the active site, via a comprehensive program of synthesis of analogues of XK469 and evaluation of the effects of structural modification(s) on solid tumor activity. The strategy formulated chose to dissect the two-dimensional parent structure into three regionsI, ring A of quinoxaline; II, the hydroquinone connector linkage; and III, the lactic acid moietyto determine the resultant in vitro and in vivo effects of chemical alterations in each region. Neither the A-ring unsubstituted nor the B-ring 3-chloro-regioisomer of XK469 showed antitumor activity. The modulating antitumor effect(s) of substituents of differing electronegativities, located at the several sites comprising the A-ring of region I, were next ascertained. Thus, a halogen substituent, located at the 7-position of a 2-{4-[(2-quinoxalinyl)oxy]phenoxy}propionic acid, generated the most highly and broadly active antitumor agents. A methyl, methoxy, or an azido substituent at this site generated a much less active structure, whereas 5-, 6-, 8-chloro-, 6-, 7-nitro, and 7-amino derivatives all proved to be essentially inactive. When the connector linkage (region II) of 1 was changed from that of a hydroquinone to either a resorcinol or a catechol derivative, all antitumor activity was lost. Of the carboxylic acid derivatives of XK469 (region III), i.e., CONH2, CONHCH3, CON(CH3)2, CONHOH, CONHNH2, CN, or CN4H (tetrazole), only the monomethyl- and N,N-dimethylamides proved to be active.

10.1021/jm0005149

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Citations (107)

Producción de semilla de maíz morado (Zea mays L) variedad LP-101 Canaán (2750 m.s.n.m) - Ayacucho

Universidad Nacional de San Cristóbal de Huamanga (2012)

Eduardo Palomino

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A Dihydropyridine Carrier System for Delivery of 2′,3′-Dideoxycytidine (DDC) to the Brain

Nucleosides and Nucleotides (1992)

Eduardo Palomino David Kessel Jerome P. Horwitz

Abstract The present study extends the dihdropyridine ⇌ pyridinium salt redox system to the delivery and sustained release of 2′,3′-dideoxycytidine (DDC) to the brains of mice in a continuing search for agents that may prove effective in reversing complicating neurological disorders of AIDS.

Delivery system

10.1080/07328319208021355

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Citations (9)