DOI: 10.1073/pnas.91.11.4708. The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.

The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.

10.1073/pnas.91.11.4708

Crossref journal-article

Proceedings of the National Academy of Sciences

Proceedings of the National Academy of Sciences (341)

Abstract

A library of 192 structurally diverse 1,4-benzodiazepine derivatives containing a variety of chemical functionalities including amides, carboxylic acids, amines, phenols, and indoles was constructed from three components, 2-aminobenzophenones, amino acids, and alkylating agents, by employing Geysen's pin apparatus [Geysen, H. M., Rodda, S. J., Mason, T. J., Tribbick, G. & Schoofs, P. G. (1987) J. Immunol. Methods 102, 259-274]. Rigorous analytical verification of the chemical integrity and yield of a representative collection of the diverse derivatives was carried out. In addition, the library of derivatives was evaluated for binding to the cholecystokinin A receptor by employing a competitive radio-ligand binding assay. This provided detailed structure versus activity relationships that were confirmed by independent large-scale synthesis and evaluation of several of the 1,4-benzodiazepine derivatives.

Bibliography

Bunin, B. A., Plunkett, M. J., & Ellman, J. A. (1994). The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library. Proceedings of the National Academy of Sciences, 91(11), 4708â4712.

Authors 3

B A Bunin (first)
M J Plunkett (additional)
J A Ellman (additional)

References 0 Referenced 239

None

Dates

Type	When
Created	19 years, 3 months ago (May 31, 2006, 8:47 a.m.)
Deposited	3 years, 4 months ago (April 13, 2022, 1:45 p.m.)
Indexed	2 months ago (July 2, 2025, 1:12 p.m.)
Issued	31 years, 3 months ago (May 24, 1994)
Published	31 years, 3 months ago (May 24, 1994)
Published Online	31 years, 3 months ago (May 24, 1994)
Published Print	31 years, 3 months ago (May 24, 1994)

Funders 0

None

BibTeX

@article{Bunin_1994, title={The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.}, volume={91}, ISSN={1091-6490}, url={http://dx.doi.org/10.1073/pnas.91.11.4708}, DOI={10.1073/pnas.91.11.4708}, number={11}, journal={Proceedings of the National Academy of Sciences}, publisher={Proceedings of the National Academy of Sciences}, author={Bunin, B A and Plunkett, M J and Ellman, J A}, year={1994}, month=may, pages={4708–4712} }

JSON

{
  "indexed": {
    "date-parts": [
      [
        2025,
        7,
        2
      ]
    ],
    "date-time": "2025-07-02T17:12:51Z",
    "timestamp": 1751476371772
  },
  "reference-count": 0,
  "publisher": "Proceedings of the National Academy of Sciences",
  "issue": "11",
  "content-domain": {
    "domain": [
      "www.pnas.org"
    ],
    "crossmark-restriction": true
  },
  "published-print": {
    "date-parts": [
      [
        1994,
        5,
        24
      ]
    ]
  },
  "abstract": "<jats:p>A library of 192 structurally diverse 1,4-benzodiazepine derivatives containing a variety of chemical functionalities including amides, carboxylic acids, amines, phenols, and indoles was constructed from three components, 2-aminobenzophenones, amino acids, and alkylating agents, by employing Geysen's pin apparatus [Geysen, H. M., Rodda, S. J., Mason, T. J., Tribbick, G. &amp; Schoofs, P. G. (1987) J. Immunol. Methods 102, 259-274]. Rigorous analytical verification of the chemical integrity and yield of a representative collection of the diverse derivatives was carried out. In addition, the library of derivatives was evaluated for binding to the cholecystokinin A receptor by employing a competitive radio-ligand binding assay. This provided detailed structure versus activity relationships that were confirmed by independent large-scale synthesis and evaluation of several of the 1,4-benzodiazepine derivatives.</jats:p>",
  "DOI": "10.1073/pnas.91.11.4708",
  "type": "journal-article",
  "created": {
    "date-parts": [
      [
        2006,
        5,
        31
      ]
    ],
    "date-time": "2006-05-31T12:47:09Z",
    "timestamp": 1149079629000
  },
  "page": "4708-4712",
  "update-policy": "http://dx.doi.org/10.1073/pnas.cm10313",
  "source": "Crossref",
  "is-referenced-by-count": 239,
  "title": "The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.",
  "prefix": "10.1073",
  "volume": "91",
  "author": [
    {
      "given": "B A",
      "family": "Bunin",
      "sequence": "first",
      "affiliation": [
        {
          "name": "Department of Chemistry, University of California at Berkeley 94720."
        }
      ]
    },
    {
      "given": "M J",
      "family": "Plunkett",
      "sequence": "additional",
      "affiliation": [
        {
          "name": "Department of Chemistry, University of California at Berkeley 94720."
        }
      ]
    },
    {
      "given": "J A",
      "family": "Ellman",
      "sequence": "additional",
      "affiliation": [
        {
          "name": "Department of Chemistry, University of California at Berkeley 94720."
        }
      ]
    }
  ],
  "member": "341",
  "published-online": {
    "date-parts": [
      [
        1994,
        5,
        24
      ]
    ]
  },
  "container-title": "Proceedings of the National Academy of Sciences",
  "original-title": [],
  "language": "en",
  "link": [
    {
      "URL": "https://pnas.org/doi/pdf/10.1073/pnas.91.11.4708",
      "content-type": "unspecified",
      "content-version": "vor",
      "intended-application": "similarity-checking"
    }
  ],
  "deposited": {
    "date-parts": [
      [
        2022,
        4,
        13
      ]
    ],
    "date-time": "2022-04-13T17:45:47Z",
    "timestamp": 1649871947000
  },
  "score": 1,
  "resource": {
    "primary": {
      "URL": "https://pnas.org/doi/full/10.1073/pnas.91.11.4708"
    }
  },
  "subtitle": [],
  "short-title": [],
  "issued": {
    "date-parts": [
      [
        1994,
        5,
        24
      ]
    ]
  },
  "references-count": 0,
  "journal-issue": {
    "issue": "11",
    "published-print": {
      "date-parts": [
        [
          1994,
          5,
          24
        ]
      ]
    }
  },
  "alternative-id": [
    "10.1073/pnas.91.11.4708"
  ],
  "URL": "http://dx.doi.org/10.1073/pnas.91.11.4708",
  "relation": {},
  "ISSN": [
    "0027-8424",
    "1091-6490"
  ],
  "subject": [],
  "container-title-short": "Proc. Natl. Acad. Sci. U.S.A.",
  "published": {
    "date-parts": [
      [
        1994,
        5,
        24
      ]
    ]
  },
  "assertion": [
    {
      "value": "1994-05-24",
      "order": 2,
      "name": "published",
      "label": "Published",
      "group": {
        "name": "publication_history",
        "label": "Publication History"
      }
    }
  ]
}