Tiostreptonhe hua kitakita taiao tino uaua e whakamahia ana hei rongoā ā-paparongoā paturopi karareheā, he pai hoki te mahi ārai-mate me te matepukupuku. I tēnei wā, kua hangaia katoatia mā te matū.
Ko te Thiostrepton, i wehea tuatahitia mai i ngā huakita i te tau 1955, he mahi paturopi rerekē tōna: ka aukati i te hanga pūmua mā te herea ki te RNA ribosomal me ōna pūmua e pā ana. Nā Dorothy Crowfoot Hodgkin, he tohunga karaihe Piritana me te toa Nobel o te tau 1964, i kitea te hanganga i te tau 1970.
Kei roto i te Thiostrepton he 10 ngā mowhiti, 11 ngā here peptide, he whānui te kore-mākū, me te 17 ngā pokapū stereo. He uaua ake anō hoki te mea he tino tairongo ki ngā waikawa me ngā kawakore. Koinei te matū matua, ā, ko te mema tino uaua o te whānau paturopi thiopeptide.
Kua hinga tēnei matū i ngā kōrero reka a te ahorangi matū a KS Nicolaou me āna hoa mahi o te Scripps Research Institute me te Whare Wānanga o California i San Diego [Angew. Chem. internationality. Editors, 43, 5087 me 5092 (2004)].
I kī a Christopher J. Moody, he Kairangahau Matua i te Tari Matū i te Whare Wānanga o Exeter, UK: "He whakahiatotanga nui tēnei, he whakatutukitanga whakamiharo hoki nā te rōpū Nicolaou." doxorubicin D.
Te kī ki te hanganga oTĪOSTREPTONko te mowhiti dehydropiperidine, e tautoko ana i te hiku didehydroalanine me ngā macrocycles e rua – he mowhiti kei roto ko te thiazoline he 26-mema me te pūnaha waikawa quinalcolic he 27-mema. Nā Nicolaou mā i hanga te mowhiti dehydropiperidine matua mai i ngā rauemi tīmatanga māmā mā te whakamahi i te tauhohenga dimerization iso-Diels–Alder biomimetic. Nā tēnei taahiraa nui i whakaū te whakaaro o te tau 1978 kia whakamahia e ngā huakita tēnei tauhohenga hei hanga i ngā paturopi thiopeptide.
I whakauruhia e Nicolaou mā ngā hoa mahi te dehydropiperidine ki roto i tētahi macrocycle kei roto i te thiazoline. I whakakotahihia e rātou tēnei macrocycle me tētahi hanganga kei roto ko te waikawa quinalcolic me tētahi matūmua hiku didehydroalanine. Kātahi ka purea e rātou te hua kia whiwhi aitiostrepton.
I kī ngā kaiarotake o ngā tuhinga e rua a te rōpū, ko te whakahiatotanga "he mahi toi e whakaatu ana i ngā hangarau hou, e whakatuwhera ana hoki i ngā pae hou mō ngā rangahau whai tikanga mō te hanganga, te mahi, me te momo mahi."
Wā tuku: Oketopa-31-2023